Selectivity data for probe BAY 1753011 and control BAY-2297
Jump to control PDSP data
BAY 1753011
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT1A | HTR1A | 46.79 | ||
| 5-HT1B | HTR1B | 4.87 | ||
| 5-HT1D | HTR1D | -18.42 | ||
| 5-HT2A | HTR2A | 0.62 | ||
| 5-HT2C | HTR2C | -15.44 | ||
| 5-HT3 | HTR3A | -4.35 | ||
| 5-HT5A | HTR5A | 3.65 | ||
| 5-HT6 | HTR6 | 17.36 | ||
| 5-HT7A | HTR7 | 17.56 | ||
| Alpha1A | ADRA1A | -2.04 | ||
| Alpha1B | ADRA1B | -5.25 | ||
| Alpha1D | ADRA1D | -0.23 | ||
| Alpha2A | ADRA2A | 8.06 | ||
| Alpha2B | ADRA2B | 16.07 | ||
| Alpha2C | ADRA2C | -2.74 | ||
| Beta1 | ADRB1 | -7.44 | ||
| Beta2 | ADRB2 | -4.34 | ||
| Beta3 | ADRB3 | -1.97 | ||
| GABAA/BZP | -64.88 | |||
| D1 | DRD1 | -6.55 | ||
| D2 | DRD2 | -5.84 | ||
| D3 | DRD3 | 19.67 | ||
| D4 | DRD4 | 19.47 | ||
| D5 | DRD5 | 1.94 | ||
| DAT | SLC6A3 | -15.11 | ||
| DOR | OPRD1 | 15.45 | ||
| H1 | HRH1 | 12.01 | ||
| H3 | HRH3 | 11.87 | ||
| H4 | HRH4 | -1.47 | ||
| KOR | OPRK1 | 62.41 | 2166.66 average (n=2) | 5.67 |
| M1 | CHRM1 | 4.34 | ||
| M2 | CHRM2 | 4.65 | ||
| M3 | CHRM3 | 28.21 | ||
| M4 | CHRM4 | -11.13 | ||
| M5 | CHRM5 | -1.80 | ||
| MOR | OPRM1 | 14.41 | ||
| NET | SLC6A2 | 71.24 | 1316.15 average (n=2) | 5.88 |
| GABA/PBR | -10.86 | |||
| SERT | SLC6A4 | 9.13 | ||
| Sigma 1 | TMEM97 | 26.97 | ||
| Sigma 2 | SIGMAR1 | 27.68 | ||
| 5-HT2B | HTR2B | 13.11 |
BAY-2297
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT2B | HTR2B | 7.98 | ||
| 5-HT1A | HTR1A | 33.31 | ||
| 5-HT1B | HTR1B | 7.15 | ||
| 5-HT1D | HTR1D | 10.09 | ||
| 5-HT2A | HTR2A | -2.02 | ||
| 5-HT2C | HTR2C | -17.44 | ||
| 5-HT3 | HTR3A | -2.44 | ||
| 5-HT5A | HTR5A | -4.02 | ||
| 5-HT6 | HTR6 | 1.09 | ||
| 5-HT7A | HTR7 | -2.00 | ||
| Alpha1A | ADRA1A | -13.76 | ||
| Alpha1B | ADRA1B | -2.47 | ||
| Alpha1D | ADRA1D | -1.97 | ||
| Alpha2A | ADRA2A | -3.35 | ||
| Alpha2B | ADRA2B | 0.10 | ||
| Alpha2C | ADRA2C | -9.85 | ||
| Beta1 | ADRB1 | -11.59 | ||
| Beta2 | ADRB2 | -12.70 | ||
| Beta3 | ADRB3 | -0.32 | ||
| GABAA/BZP | -3.13 | |||
| D1 | DRD1 | -16.95 | ||
| D2 | DRD2 | -8.61 | ||
| D3 | DRD3 | 18.30 | ||
| D4 | DRD4 | -4.70 | ||
| D5 | DRD5 | 19.59 | ||
| DAT | SLC6A3 | 4.92 | ||
| DOR | OPRD1 | 12.45 | ||
| H1 | HRH1 | 28.49 | ||
| H3 | HRH3 | 5.05 | ||
| H4 | HRH4 | 0.51 | ||
| KOR | OPRK1 | 3.83 | ||
| M1 | CHRM1 | -11.09 | ||
| M2 | CHRM2 | -9.34 | ||
| M3 | CHRM3 | -4.25 | ||
| M4 | CHRM4 | -9.78 | ||
| M5 | CHRM5 | -5.11 | ||
| MOR | OPRM1 | 6.13 | ||
| NET | SLC6A2 | 11.01 | ||
| GABA/PBR | -0.38 | |||
| SERT | SLC6A4 | 14.08 | ||
| Sigma 1 | TMEM97 | 24.06 | ||
| Sigma 2 | SIGMAR1 | 9.61 |
BAY 1753011
Results are significant for > 50 % inhibition.
Conclusion: Clean panel except for OXTR with IC50 = 15.5 nM at 1 µM.
| Target protein | HGNC name | Species | Cmp. conc. | % inhibition | IC50 [µM] | Ki [µM] | Reference compound name | Reference compound IC50 [nM] | Assay ID |
|---|---|---|---|---|---|---|---|---|---|
| Sigma 2 | TMEM97 | Rattus sp. | 10 µM | 5.0 | Ifenprodil | 8.00 | 278200 | ||
| Adenosine A1 | ADORA1 | Homo sapiens | 10 µM | 26.0 | R(-)-PIA | 830.00 | 200510 | ||
| Adenosine A2A | ADORA2A | Homo sapiens | 10 µM | 4.0 | CGS-21680 | 130.00 | 200610 | ||
| Adenosine A3 | ADORA3 | Homo sapiens | 10 µM | 16.0 | IB-MECA | 0.78 | 200720 | ||
| Adrenergic alpha1A | ADRA1A | Rattus sp. | 10 µM | 23.0 | Prazosin | 0.69 | 203100 | ||
| Adrenergic alpha1B | ADRA1B | Rattus sp. | 10 µM | 3.0 | Prazosin | 0.27 | 203200 | ||
| Adrenergic alpha1D | ADRA1D | Homo sapiens | 10 µM | 1.0 | Prazosin | 0.88 | 203400 | ||
| Adrenergic alpha2A | ADRA2A | Homo sapiens | 10 µM | 3.0 | Yohimbine | 1.80 | 203630 | ||
| Adrenergic beta1 | ADRB1 | Homo sapiens | 10 µM | 5.0 | S(-)-Propranolol | 2.50 | 204010 | ||
| Adrenergic beta2 | ADRB2 | Homo sapiens | 10 µM | 9.0 | S(-)-Propranolol | 0.78 | 204110 | ||
| Androgen (Testosterone) AR | AR | Homo sapiens | 10 µM | 12.0 | Testosterone | 2.10 | 206000 | ||
| Bradykinin B1 | BDKRB1 | Homo sapiens | 10 µM | 0.0 | (Des-Arg10)-Kallidin | 0.87 | 212510 | ||
| Bradykinin B2 | BDKRB2 | Homo sapiens | 10 µM | 1.0 | Bradykinin | 1.80 | 212620 | ||
| Calcium Channel L-Type, Benzothiazepine | CACNA1C | Rattus sp. | 10 µM | 35.0 | Diltiazem | 0.04 | 214510 | ||
| Calcium Channel L-Type, Dihydropyridine | CACNA1C | Rattus sp. | 10 µM | 37.0 | Nitrendipine | 0.72 | 214600 | ||
| Calcium Channel N-Type | CACNA1B | Rattus sp. | 10 µM | -2.0 | ω-Conotoxin GVIA | 0.03 | 216000 | ||
| Cannabinoid CB1 | CNR1 | Homo sapiens | 10 µM | 34.0 | R(+)-WIN-55,212-2 | 200.00 | 217030 | ||
| Dopamine D1 | DRD1 | Homo sapiens | 10 µM | 1.0 | R(+)-SCH-23390 | 1.40 | 219500 | ||
| Dopamine D2S | DRD2 | Homo sapiens | 10 µM | 14.0 | Spiperone | 0.25 | 219700 | ||
| Dopamine D3 | DRD3 | Homo sapiens | 10 µM | 26.0 | Spiperone | 0.36 | 219800 | ||
| Dopamine D4.2 | DRD4 | Homo sapiens | 10 µM | 3.0 | Spiperone | 29.00 | 219900 | ||
| Endothelin ETA | EDNRA | Homo sapiens | 10 µM | 18.0 | Endothelin-1 | 0.23 | 224010 | ||
| Endothelin ETB | EDNRB | Homo sapiens | 10 µM | 5.0 | Endothelin-1 | 0.13 | 224110 | ||
| Epidermal Growth Factor (EGF) | EGFR | Homo sapiens | 10 µM | 14.0 | EGF (human) | 1.60 | 225510 | ||
| Estrogen ERalpha | ESR1 | Homo sapiens | 10 µM | 8.0 | Diethylstilbestrol | 0.77 | 226010 | ||
| GABAA, Muscimol, Central | Rattus sp. | 10 µM | -2.0 | 4-aminobutyric acid | 0.03 | 226500 | |||
| GABAA, Flunitrazepam, Central | Rattus sp. | 10 µM | -1.0 | Hydrogen diazepam chloride | 0.02 | 226600 | |||
| GABAB1A | GABBR1 | Homo sapiens | 10 µM | -4.0 | Cgp-54626 | 6.40 | 228610 | ||
| Glucocorticoid | NR3C1 | Homo sapiens | 10 µM | 1.0 | Dexamethasone | 3.80 | 232030 | ||
| Glutamate, Kainate | GRIK2 | Rattus sp. | 10 µM | -4.0 | 232700 | ||||
| Glutamate, NMDA, Agonism | Rattus sp. | 10 µM | 2.0 | L-Glutamic acid | 410.00 | 232810 | |||
| Glutamate, NMDA, Glycine | Rattus sp. | 10 µM | -10.0 | MDL 105,519 | 22.00 | 232910 | |||
| Glutamate, NMDA, Phencyclidine | Rattus sp. | 10 µM | 14.0 | Dizolcipine ((+)-MK-801) | 5.10 | 233000 | |||
| Histamine H1 | HRH1 | Homo sapiens | 10 µM | -1.0 | Pyrilamine | 3.30 | 239610 | ||
| Histamine H2 | HRH2 | Homo sapiens | 10 µM | -17.0 | Tiotidine | 22.00 | 239710 | ||
| Histamine H3 | HRH3 | Homo sapiens | 10 µM | -1.0 | R(-)-alpha-Methylhistamine (RAMH) | 2.30 | 239820 | ||
| Imidazoline I2, Central | Rattus sp. | 10 µM | 21.0 | Idazoxan | 12.00 | 241000 | |||
| Interleukin IL-1 | Mus musculus | 10 µM | 15.0 | IL-1 beta | 0.19 | 243520 | |||
| Leukotriene, Cysteinyl CysLT1 | CYSLTR1 | Homo sapiens | 10 µM | 5.0 | Leukotriene D4 | 0.70 | 250460 | ||
| Melatonin MT1 | MTNR1A | Homo sapiens | 10 µM | -6.0 | Melatonin | 0.21 | 251600 | ||
| Muscarinic M1 | CHRM1 | Homo sapiens | 10 µM | -5.0 | 4-DAMP | 4.50 | 252610 | ||
| Muscarinic M2 | CHRM2 | Homo sapiens | 10 µM | 7.0 | 4-DAMP | 55.00 | 252710 | ||
| Muscarinic M3 | CHRM3 | Homo sapiens | 10 µM | 8.0 | 4-DAMP | 5.10 | 252810 | ||
| Neuropeptide Y Y1 | NPY1R | Homo sapiens | 10 µM | 11.0 | Neuropeptide Y (human, rat) | 0.22 | 257010 | ||
| Neuropeptide Y Y2 | NPY2R | Homo sapiens | 10 µM | 6.0 | Neuropeptide Y (13-36) (porcine) | 0.21 | 257110 | ||
| Nicotinic Acetylcholine | Homo sapiens | 10 µM | -6.0 | Epibatidine | 0.08 | 258590 | |||
| Nicotinic Acetylcholine D1, Bungarotoxin | CHRNA1 | Homo sapiens | 10 µM | -25.0 | alpha-Bungarotoxin | 1.10 | 258700 | ||
| Opiate delta1 (OP1, DOP) | OPRD1 | Homo sapiens | 10 µM | 4.0 | Naltrindole | 0.91 | 260130 | ||
| Opiate kappa (OP2, KOP) | OPRK1 | Homo sapiens | 10 µM | 19.0 | U-69593 | 16.00 | 260210 | ||
| Opiate µ (OP3, MOP) | OPRM1 | Homo sapiens | 10 µM | 24.0 | DAMGO | 20.00 | 260410 | ||
| Phorbol Ester | Mus musculus | 10 µM | 3.0 | Phorbol myristate acetate | 0.79 | 264500 | |||
| Platelet Activating Factor (PAF) | PTAFR | Homo sapiens | 10 µM | 17.0 | PAF | 0.28 | 265010 | ||
| Potassium Channel [KATP] | KCNJ11 | Cricetinae | 10 µM | 18.0 | Glyburide | 5.70 | 265600 | ||
| Potassium Channel hERG | KCNH2 | Homo sapiens | 10 µM | -3.0 | Astemizole | 265900 | |||
| Prostanoid EP4 | PTGER4 | Homo sapiens | 10 µM | 16.0 | Prostaglandin E2 | 1.10 | 268420 | ||
| Purinergic P2X | Oryctolagus cuniculus | 10 µM | 18.0 | alpha,beta-Methylene ATP | 82.00 | 268700 | |||
| Purinergic P2Y | Rattus sp. | 10 µM | 0.0 | ATP | 18.00 | 268810 | |||
| Rolipram | Rattus sp. | 10 µM | -2.0 | Rolipram | 5.70 | 270000 | |||
| Serotonin (5-Hydroxytryptamine) 5-HT1A | HTR1A | Homo sapiens | 10 µM | -2.0 | Metergoline | 4.10 | 271110 | ||
| Serotonin (5-Hydroxytryptamine) 5-HT2B | HTR2B | Homo sapiens | 10 µM | 52.0 | Ketanserin | 290.00 | 271700 | ||
| Serotonin (5-Hydroxytryptamine) 5-HT3 | HTR3A | Homo sapiens | 10 µM | -2.0 | MDL-72222 | 11.00 | 271910 | ||
| Sigma 1 | SIGMAR1 | Homo sapiens | 10 µM | 15.0 | Haloperidol | 21.00 | 278110 | ||
| Sodium Channel, Site 2 | Rattus sp. | 10 µM | 42.0 | Dibucaine | 61.00 | 279510 | |||
| Tachykinin NK1 | TACR1 | Homo sapiens | 10 µM | 20.0 | L-703606 | 3.60 | 255520 | ||
| Thyroid Hormone | Rattus sp. | 10 µM | 6.0 | Liothyronine | 0.03 | 285900 | |||
| Transporter, Dopamine (DAT) | SLC6A3 | Homo sapiens | 10 µM | 4.0 | GBR-12909 | 1.70 | 220320 | ||
| Transporter, GABA | Rattus sp. | 10 µM | 8.0 | NO-711 | 200.00 | 226400 | |||
| Transporter, Norepinephrine (NET) | SLC6A2 | Homo sapiens | 10 µM | 62.0 | Desipramine | 0.93 | 204410 | ||
| Transporter, Serotonin (5- Hydroxytryptamine) (SERT) | SLC6A4 | Homo sapiens | 10 µM | 6.0 | Fluoxetine | 8.60 | 274030 | ||
| Oxytocin | OXTR | Homo sapiens | 0.0001 µM | 3.0 | 0.02 | 0.01 | Oxytocin | 950.00 | 260900 |
| Adrenergic alpha2B | ADRA2B | Homo sapiens | 10 µM | 8.0 | Yohimbine | 14.00 | 203710 | ||
| Adrenergic alpha2C | ADRA2C | Homo sapiens | 10 µM | 11.0 | Yohimbine | 2.00 | 203810 | ||
| Adrenergic beta3 | ADRB3 | Homo sapiens | 10 µM | -10.0 | Alprenolol | 180.00 | 204200 | ||
| Angiotensin AT2 | AGTR2 | Homo sapiens | 10 µM | 4.0 | Saralasin | 0.35 | 210120 | ||
| Atrial Natriuretic Factor (ANF) | Cavia porcellus | 10 µM | 1.0 | ANF (rat) | 0.40 | 211000 | |||
| Calcitonin | CALCR | Homo sapiens | 10 µM | -7.0 | Calcitonin (salmon) | 0.39 | 213610 | ||
| Calcium Channel L-Type, Phenylalkylamine | CACNA1C | Rattus sp. | 10 µM | 22.0 | Methoxyverapamil (D-600) | 22.00 | 215000 | ||
| Chemokine CCR2B | CCR2 | Homo sapiens | 10 µM | 2.0 | MCP-1 | 0.07 | 217550 | ||
| Chemokine CCR4 | CCR4 | Homo sapiens | 10 µM | -2.0 | 217660 | ||||
| Chemokine CCR5 | CCR5 | Homo sapiens | 10 µM | -3.0 | 217720 | ||||
| Chemokine CXCR2 (IL-8RB) | CXCR2 | Homo sapiens | 10 µM | -6.0 | IL-8 | 0.18 | 244500 | ||
| Cholecystokinin CCK1 (CCKA) | CCKAR | Homo sapiens | 10 µM | 15.0 | Devazepide (L-364,718) | 0.18 | 218020 | ||
| Dopamine D2L | DRD2 | Homo sapiens | 10 µM | 14.0 | Spiperone | 219600 | |||
| GABAA, Chloride Channel, TBOB | Rattus sp. | 10 µM | 30.0 | Picrotoxin | 270.00 | 226810 | |||
| Glutamate, AMPA | Rattus sp. | 10 µM | 2.0 | L-Glutamic acid | 320.00 | 232600 | |||
| Glycine, Strychnine-Sensitive | Rattus sp. | 10 µM | 12.0 | (-)-Strychnine | 8.90 | 239000 | |||
| Insulin | INSR | Rattus sp. | 10 µM | -1.0 | Insulin | 6.10 | 243000 | ||
| Melanocortin MC3 | MC3R | Homo sapiens | 10 µM | 6.0 | NDP-alpha-MSH | 0.15 | 251300 | ||
| Melanocortin MC4 | MC4R | Homo sapiens | 10 µM | 4.0 | NDP-alpha-MSH | 0.22 | 251350 | ||
| Melanocortin MC5 | MC5R | Homo sapiens | 10 µM | 13.0 | NDP-alpha-MSH | 0.48 | 251400 | ||
| Muscarinic M4 | CHRM4 | Homo sapiens | 10 µM | 7.0 | 4-DAMP | 15.00 | 252910 | ||
| Muscarinic M5 | CHRM5 | Homo sapiens | 10 µM | 6.0 | 4-DAMP | 3.20 | 253010 | ||
| Platelet-Derived Growth Factor (PDGF) | Mus musculus | 10 µM | 5.0 | 265200 | |||||
| Progesterone PR-B | PGR | Homo sapiens | 10 µM | 0.0 | Progesterone | 1.50 | 268020 | ||
| Serotonin (5-Hydroxytryptamine) 5-HT1B | HTR1B | Rattus sp. | 10 µM | -5.0 | Serotonin (5-HT) | 5.70 | 271200 | ||
| Serotonin (5-Hydroxytryptamine) 5-HT2C | HTR2C | Homo sapiens | 10 µM | 20.0 | SBZ4Z084 | 1.00 | 271800 | ||
| Serotonin (5-Hydroxytryptamine) 5-HT4 | HTR4 | Cavia porcellus | 10 µM | 19.0 | RS-23597-190 | 90.00 | 272000 | ||
| Serotonin (5-Hydroxytryptamine) 5-HT6 | HTR6 | Homo sapiens | 10 µM | 4.0 | Methiothepin | 2.80 | 272200 | ||
| Tachykinin NK2 | TACR2 | Homo sapiens | 10 µM | 30.0 | MEN-10,376 | 110.00 | 255600 | ||
| Transporter, Adenosine | Cavia porcellus | 10 µM | 21.0 | Nitrobenzylthioinosine | 0.85 | 202000 | |||
| Tumor Necrosis Factor (TNF), Non-Selective | Homo sapiens | 10 µM | -1.0 | 286510 | |||||
| Vasoactive Intestinal Peptide VIP1 | VIPR1 | Homo sapiens | 10 µM | 10.0 | VIP | 0.13 | 287010 | ||
| Vasopressin V1A | AVPR1A | Homo sapiens | 0.01 µM | 65.0 | 0.01 | 0.00 | (Arg8)-Vasopressin | 0.33 | 287530 |
| Vasopressin V1B | AVPR1B | Homo sapiens | 0.001 µM | 6.0 | 10.00 | (Arg8)-Vasopressin | 0.66 | 287560 |
BAY-2297
Conclusion: Clean panel.
| Target protein | HGNC name | Species | Cmp. conc. | % inhibition | Reference compound name | Reference compound IC50 [nM] | Assay ID |
|---|---|---|---|---|---|---|---|
| Adenosine A1 | ADORA1 | Homo sapiens | 10 µM | 8.0 | R(-)-PIA | 830.0 | 200510 |
| Adenosine A2A | ADORA2A | Homo sapiens | 10 µM | 1.0 | CGS-21680 | 130.0 | 200610 |
| Adenosine A3 | ADORA3 | Homo sapiens | 10 µM | 7.0 | IB-MECA | 0.8 | 200720 |
| Adrenergic alpha1A | ADRA1A | Homo sapiens | 10 µM | 3.0 | Prazosin hydrochloride | 0.9 | 203110 |
| Adrenergic alpha2A | ADRA2A | Homo sapiens | 10 µM | 5.0 | Yohimbine | 1.8 | 203630 |
| Adrenergic alpha2B | ADRA2B | Homo sapiens | 10 µM | 2.0 | Yohimbine | 14.0 | 203710 |
| Adrenergic alpha2C | ADRA2C | Homo sapiens | 10 µM | -3.0 | Yohimbine | 2.0 | 203810 |
| Adrenergic beta1 | ADRB1 | Homo sapiens | 10 µM | 5.0 | S(-)-Propranolol | 2.5 | 204010 |
| Adrenergic beta2 | ADRB2 | Homo sapiens | 10 µM | 0.0 | S(-)-Propranolol | 0.8 | 204110 |
| Adrenergic beta3 | ADRB3 | Homo sapiens | 10 µM | 6.0 | Alprenolol | 180.0 | 204200 |
| Androgen (Testosterone) AR | AR | Homo sapiens | 10 µM | 9.0 | Testosterone | 2.1 | 206000 |
| Angiotensin AT1 | AGTR1 | Homo sapiens | 10 µM | -6.0 | Saralasin | 0.9 | 210030 |
| Angiotensin AT2 | AGTR2 | Homo sapiens | 10 µM | -3.0 | Saralasin | 0.4 | 210120 |
| Bradykinin B1 | BDKRB1 | Homo sapiens | 10 µM | -3.0 | (Des-Arg10)-Kallidin | 0.3 | 212520 |
| Bradykinin B2 | BDKRB2 | Homo sapiens | 10 µM | -10.0 | Bradykinin | 1.8 | 212620 |
| Cannabinoid CB1 | CNR1 | Homo sapiens | 10 µM | 19.0 | SR141716A | 4.0 | 217050 |
| Cannabinoid CB2 | CNR2 | Homo sapiens | 10 µM | 14.0 | R(+)-WIN-55,212-2 | 5.8 | 217100 |
| Dopamine D1 | DRD1 | Homo sapiens | 10 µM | -6.0 | R(+)-SCH-23390 | 1.4 | 219500 |
| Dopamine D2L | DRD2 | Homo sapiens | 10 µM | 16.0 | Spiperone | 219600 | |
| Dopamine D2S | DRD2 | Homo sapiens | 10 µM | -3.0 | Spiperone | 0.3 | 219700 |
| Dopamine D3 | DRD3 | Homo sapiens | 10 µM | -8.0 | Spiperone | 0.4 | 219800 |
| Endothelin ETA | EDNRA | Homo sapiens | 10 µM | -3.0 | Endothelin-1 | 0.2 | 224010 |
| Endothelin ETB | EDNRB | Homo sapiens | 10 µM | 1.0 | Endothelin-1 | 0.1 | 224110 |
| Estrogen ERalpha | ESR1 | Homo sapiens | 10 µM | 4.0 | Diethylstilbestrol | 0.8 | 226010 |
| GABAA, Chloride Channel, TBOB | Rattus sp. | 10 µM | 12.0 | Picrotoxin | 270.0 | 226810 | |
| GABAA, Flunitrazepam, Central | Rattus sp. | 10 µM | -1.0 | Hydrogen diazepam chloride | 0.0 | 226600 | |
| GABAB, Non-Selective | GABBR1 | Rattus sp. | 10 µM | 8.0 | CGP-546Z6 | 1.8 | 228510 |
| Glucocorticoid | NR3C1 | Homo sapiens | 10 µM | 32.0 | Dexamethasone | 3.8 | 232030 |
| Glutamate, AMPA | Rattus sp. | 10 µM | 3.0 | L-Glutamic acid | 320.0 | 232600 | |
| Glutamate, Kainate | Rattus sp. | 10 µM | -11.0 | L-Glutamic acid hydrochloride | 160.0 | 232710 | |
| Glutamate, NMDA, Agonism | Rattus sp. | 10 µM | -8.0 | L-Glutamic acid | 410.0 | 232810 | |
| Glutamate, NMDA, Glycine | Rattus sp. | 10 µM | -4.0 | MDL 105,519 | 22.0 | 232910 | |
| Growth Hormone Secretagogue (GHS, Ghrelin) | GHSR | Homo sapiens | 10 µM | 25.0 | Ghrelin (human) | 0.1 | 239300 |
| Histamine H1 | HRH1 | Homo sapiens | 10 µM | 9.0 | Pyrilamine | 3.3 | 239610 |
| Histamine H2 | HRH2 | Homo sapiens | 10 µM | -13.0 | Tiotidine | 22.0 | 239710 |
| Histamine H3 | HRH3 | Homo sapiens | 10 µM | -12.0 | R(-)-alpha-Methylhistamine (RAMH) | 2.3 | 239820 |
| Insulin | INSR | Rattus sp. | 10 µM | 1.0 | Insulin | 6.1 | 243000 |
| Motilin | MLNR | Homo sapiens | 10 µM | 12.0 | Motilin porcine | 0.5 | 252200 |
| Muscarinic M1 | CHRM1 | Homo sapiens | 10 µM | 1.0 | 4-DAMP | 4.5 | 252610 |
| Muscarinic M2 | CHRM2 | Homo sapiens | 10 µM | 17.0 | 4-DAMP | 55.0 | 252710 |
| Muscarinic M3 | CHRM3 | Homo sapiens | 10 µM | 4.0 | 4-DAMP | 5.1 | 252810 |
| Muscarinic M4 | CHRM4 | Homo sapiens | 10 µM | 0.0 | 4-DAMP | 15.0 | 252910 |
| Nicotinic Acetylcholine alpha3beta4 |
CHRNA3 CHRNB4 |
Homo sapiens | 10 µM | -5.0 | Epibatidine | 0.1 | 258730 |
| Opiate delta1 (OP1, DOP) | OPRD1 | Homo sapiens | 10 µM | 2.0 | Naltrindole | 0.9 | 260130 |
| Opiate kappa (OP2, KOP) | OPRK1 | Homo sapiens | 10 µM | 10.0 | U-69593 | 16.0 | 260210 |
| Opiate µ (OP3, MOP) | OPRM1 | Homo sapiens | 10 µM | -6.0 | DAMGO | 20.0 | 260410 |
| Oxytocin | OXTR | Homo sapiens | 10 µM | 12.0 | Oxytocin | 950.0 | 260900 |
| Progesterone PR-B | PGR | Homo sapiens | 10 µM | 25.0 | R-5020 | 0.5 | 299005 |
| Purinergic P2X | Rattus sp. | 10 µM | -5.0 | alpha,beta-Methylene ATP | 11.0 | 299036 | |
| Purinergic P2Y | Rattus sp. | 10 µM | 4.0 | 2-Methylthio-ATP | 85.0 | 268820 | |
| Serotonin (5-Hydroxytryptamine) 5-HT1A | HTR1A | Homo sapiens | 10 µM | -1.0 | Metergoline | 4.1 | 271110 |
| Serotonin (5-Hydroxytryptamine) 5-HT2A | HTR2A | Homo sapiens | 10 µM | -2.0 | Ketanserin | 0.7 | 271650 |
| Serotonin (5-Hydroxytryptamine) 5-HT2B | HTR2B | Homo sapiens | 10 µM | 12.0 | Ketanserin | 290.0 | 271700 |
| Serotonin (5-Hydroxytryptamine) 5-HT2C | HTR2C | Homo sapiens | 10 µM | -1.0 | SBZ4Z084 | 1.0 | 271800 |
| Transporter, Adenosine | Homo sapiens | 10 µM | 10.0 | NBTI | 0.6 | 202020 | |
| Transporter, Dopamine (DAT) | SLC6A3 | Homo sapiens | 10 µM | 19.0 | GBR-12909 | 1.7 | 220320 |
| Transporter, GABA | Rattus sp. | 10 µM | 9.0 | NO-711 | 200.0 | 226400 | |
| Transporter, Norepinephrine (NET) | SLC6A2 | Homo sapiens | 10 µM | 8.0 | Desipramine | 0.9 | 204410 |
| Transporter, Serotonin (5- Hydroxytryptamine) (SERT) | SLC6A4 | Homo sapiens | 10 µM | 1.0 | Fluoxetine | 8.6 | 274030 |
| Vasopressin V1A | AVPR1A | Homo sapiens | 10 µM | 28.0 | (Arg8)-Vasopressin | 0.3 | 287530 |
| Vasopressin V1B | AVPR1B | Homo sapiens | 10 µM | 7.0 | (Arg8)-Vasopressin | 0.7 | 287560 |
| Vasopressin V2 | AVPR2 | Homo sapiens | 10 µM | 29.0 | (Arg8)-Vasopressin | 4.5 | 287610 |
BAY 1753011
Results are significant for > 50 % inhibition. Where presented, IC50 values were determined by a non-linear, least squares regression analysis using MathIQTM (ID Business Solutions Ltd., UK).
Conclusion: Clean panel.
| Target protein | HGNC name | Species | Cmp. conc. | % inhibition | Reference compound name | Reference compound IC50 [µM] | Assay ID |
|---|---|---|---|---|---|---|---|
| Aldose Reductase | AKR1B1 | Rattus sp. | 10 µM | 6.0 | Quercitrin | 0.56 | 107000 |
| ATPase, Na+/K+, Heart | Sus scrofa | 10 µM | 0.0 | Ouabain | 2.00 | 107710 | |
| Beta-Lactamase | Bacteria | 10 µM | -17.0 | CLAVULANIC ACID | 11.00 | 126000 | |
| Carbonic Anhydrase II | CA2 | Homo sapiens | 10 µM | -4.0 | Acetazolamide | 0.03 | 112020 |
| Cholinesterase, Acetyl, ACES | ACHE | Homo sapiens | 10 µM | 2.0 | Physostigmine | 0.12 | 104010 |
| Cyclooxygenase COX-1 | PTGS1 | Homo sapiens | 10 µM | -3.0 | Indomethacin | 0.04 | 116020 |
| Cyclooxygenase COX-2 | PTGS2 | Homo sapiens | 10 µM | -12.0 | Rofecoxib | 0.17 | 118010 |
| HMG-CoA Reductase | HMGCR | Homo sapiens | 10 µM | 9.0 | Lovastatin | 0.07 | 124010 |
| Leukotriene LTC4 Synthase | LTC4S | Cavia porcellus | 10 µM | 13.0 | Sulfasalazine | 87.00 | 132000 |
| Lipoxygenase 15-LO | ALOX15 | Oryctolagus cuniculus | 10 µM | 4.0 | 138000 | ||
| Monoamine Oxidase MAO-A | MAOA | Homo sapiens | 10 µM | -3.0 | Clorgyline | 0.00 | 140010 |
| Nitric Oxide Synthase, Inducible (iNOS) | NOS2 | Mus musculus | 10 µM | -1.0 | S-Methylisothiourea | 2.30 | 144000 |
| Nitric Oxide Synthase, Neuronal (nNOS) | NOS1 | Rattus sp. | 10 µM | 10.0 | S-methylisothiourea | 142000 | |
| Peptidase, Angiotensin Converting Enzyme | ACE | Oryctolagus cuniculus | 10 µM | 2.0 | Captopril | 0.01 | 107300 |
| Peptidase, CASP1 (Caspase 1) | CASP1 | Homo sapiens | 10 µM | 0.0 | Ac-YVAD-CHO | 0.03 | 163000 |
| Peptidase, CTSG (Cathepsin G) | CTSG | Homo sapiens | 10 µM | 0.0 | Chymostatin | 2.10 | 112510 |
| Peptidase, ELA2 (Neutrophil Elastase 2) | ELANE | Homo sapiens | 10 µM | 1.0 | N-MeOSuc-Ala-Ala-Pro- Val-Chloromethylketone | 0.07 | 166010 |
| Peptidase, Matrix Metalloproteinase-1 (MMP-1) | MMP1 | Homo sapiens | 10 µM | 3.0 | GM-6001 | 114110 | |
| Peptidase, Matrix Metalloproteinase-9 (MMP-9) | MMP9 | Homo sapiens | 10 µM | -2.0 | GM-6001 | 0.00 | 114910 |
| Phosphodiesterase PDE3 | Homo sapiens | 10 µM | 0.0 | Cilostamide | 0.05 | 152000 | |
| Phosphodiesterase PDE4 | Homo sapiens | 10 µM | -4.0 | Ro 20-1724 | 1.10 | 154000 | |
| Phosphodiesterase PDE5 | PDE5A | Homo sapiens | 10 µM | -10.0 | Zaprinast | 156000 | |
| Protein Serine/Threonine Kinase, MAPK1 (ERK2) | MAPK1 | Homo sapiens | 10 µM | -2.0 | Staurosporine | 0.47 | 171120 |
| Protein Serine/Threonine Kinase, MAPK14 (p38α) | MAPK14 | Homo sapiens | 10 µM | -1.0 | SB-Z0Z190 | 0.02 | 176610 |
| Protein Serine/Threonine Kinase, MAPK3 (ERK1) | MAPK3 | Homo sapiens | 10 µM | -7.0 | Staurosporine | 1.60 | 171000 |
| Protein Serine/Threonine Kinase, PRKCA (PKCα) | PRKCA | Homo sapiens | 10 µM | -2.0 | Staurosporine | 0.00 | 180010 |
| Protein Serine/threonine Phosphatase, PPP3CA (Calcineurin, PP2B) | PPP3CA | Homo sapiens | 10 µM | 32.0 | (NH4)6Mo7O24 | 25.00 | 188020 |
| Protein Tyrosine Kinase, EGF Receptor | EGFR | Homo sapiens | 10 µM | -6.0 | 170020 | ||
| Protein Tyrosine Kinase, ERBB2 (HER2) | ERBB2 | Homo sapiens | 10 µM | 15.0 | Staurosporine | 1.30 | 174020 |
| Protein Tyrosine Kinase, Fyn | FYN | Homo sapiens | 10 µM | -6.0 | Staurosporine | 0.20 | 172020 |
| Protein Tyrosine Kinase, LCK | LCK | Homo sapiens | 10 µM | -9.0 | TC-S 7003 | 0.06 | 176020 |
| Protein Tyrosine Phosphatase, PTPRC (CD45) | PTPRC | Homo sapiens | 10 µM | 0.0 | (NH4)6Mo7O24 | 190010 | |
| Thromboxane Synthase | TBXAS1 | Homo sapiens | 10 µM | -6.0 | 1-(7-Carboxyheptyl)-Imidazole | 0.01 | 194020 |
BAY-2297
Conclusion: Clean panel.
| Target protein | HGNC name | Species | Cmp. conc. | % inhibition | Reference compound name | Reference compound IC50 [µM] | Assay ID |
|---|---|---|---|---|---|---|---|
| Aldose Reductase | AKR1B1 | Homo sapiens | 10 µM | 15.0 | Quercitrin | 3.6 | 107010 |
| ATPase, Na+/K+, Heart | Sus scrofa | 10 µM | -1.0 | Ouabain | 2.0 | 107710 | |
| Carbonic Anhydrase II | CA2 | Homo sapiens | 10 µM | -1.0 | Acetazolamide | 0.0 | 112020 |
| Cholinesterase, Acetyl, ACES | ACHE | Homo sapiens | 10 µM | 2.0 | Physostigmine | 0.1 | 104010 |
| Cyclooxygenase COX-1 | PTGS1 | Homo sapiens | 10 µM | 11.0 | Indomethacin | 0.0 | 116030 |
| Cyclooxygenase COX-2 | PTGS2 | Homo sapiens | 10 µM | 0.0 | Rofecoxib | 0.4 | 118030 |
| HMG-CoA Reductase | HMGCR | Homo sapiens | 10 µM | -18.0 | Lovastatin | 0.1 | 124010 |
| Leukotriene LTC4 Synthase | LTC4S | Cavia porcellus | 10 µM | 6.0 | Sulfasalazine | 87.0 | 132000 |
| 15-LOX-2 Lipoxygenase | ALOX15B | Homo sapiens | 10 µM | -3.0 | 2-TEDC | 0.2 | 199020 |
| Monoamine Oxidase MAO-A | MAOA | Homo sapiens | 10 µM | 2.0 | Clorgyline | 0.0 | 140010 |
| Monoamine Oxidase MAO-B | MAOB | Homo sapiens | 10 µM | 28.0 | R(-)-Deprenyl | 0.0 | 140120 |
| Nitric Oxide Synthase, Neuronal (nNOS) | NOS1 | Rattus sp. | 10 µM | -6.0 | S-methylisothiourea | 1.1 | 142000 |
| Nitric Oxide Synthase, Inducible (iNOS) | NOS2 | Mus musculus | 10 µM | 5.0 | AMT | 0.0 | 199010 |
| ACE Angiotensin-Converting Metallo Peptidase | ACE | Homo sapiens | 10 µM | -16.0 | Captopril | 0.0 | 107310 |
| PDE3A Phosphodiesterase | PDE3A | Homo sapiens | 10 µM | -6.0 | Cilostamide | 0.1 | 152300 |
| Phosphodiesterase PDE4D2 | PDE4D | Homo sapiens | 10 µM | 4.0 | Rolipram | 0.1 | 154420 |
| PDE5A Phosphodiesterase | PDE5A | Homo sapiens | 10 µM | 31.0 | Zaprinast | 0.2 | 156020 |
| Thromboxane Synthase | TBXAS1 | Homo sapiens | 10 µM | 12.0 | 1-(7-Carboxyheptyl)-Imidazole | 0.0 | 194020 |
BAY 1753011
The panel was screened at an ATP conc. of 10 µM.
Conclusion: Closest off-targets is NEK3 (60.98 % inhibition).
| Target protein | HGNC name | Species | % inhibition at 10 µM |
|---|---|---|---|
| AAK1(h) | AAK1 | Homo sapiens | -9.0 |
| Abl(h) | ABL1 | Homo sapiens | -13.3 |
| ACK1(h) | TNK2 | Homo sapiens | -1.3 |
| ACTR2(h) | ACTR2 | Homo sapiens | 5.4 |
| ALK(h) | ALK | Homo sapiens | -3.8 |
| ALK1(h) | ACVRL1 | Homo sapiens | -9.7 |
| ALK2(h) | ACVR1 | Homo sapiens | -2.5 |
| ALK4(h) | ACVR1B | Homo sapiens | 4.0 |
| ALK6(h) | BMPR1B | Homo sapiens | -1.0 |
| AMPKalpha1(h) | PRKAA1 | Homo sapiens | -4.1 |
| AMPKalpha2(h) | PRKAA2 | Homo sapiens | -11.1 |
| A-Raf(h) | ARAF | Homo sapiens | 1.1 |
| Arg(h) | ABL2 | Homo sapiens | -0.7 |
| ARK5(h) | NUAK1 | Homo sapiens | -3.6 |
| ASK1(h) | MAP3K5 | Homo sapiens | -8.6 |
| Aurora-A(h) | AURKA | Homo sapiens | 11.2 |
| Aurora-B(h) | AURKB | Homo sapiens | -25.0 |
| Aurora-C(h) | AURKC | Homo sapiens | -12.1 |
| Axl(h) | AXL | Homo sapiens | 2.0 |
| BIKe(h) | BMP2K | Homo sapiens | -0.7 |
| Blk(h) | BLK | Homo sapiens | -13.6 |
| BMPR2(h) | BMPR2 | Homo sapiens | 11.1 |
| Bmx(h) | BMX | Homo sapiens | -9.5 |
| B-Raf(h) | BRAF | Homo sapiens | -4.0 |
| BRK(h) | PTK6 | Homo sapiens | -3.8 |
| BrSK1(h) | BRSK1 | Homo sapiens | -5.4 |
| BrSK2(h) | BRSK2 | Homo sapiens | -4.8 |
| BTK(h) | BTK | Homo sapiens | -11.1 |
| CaMKI(h) | CAMK1 | Homo sapiens | -5.2 |
| CaMKIbeta(h) | PNCK | Homo sapiens | -13.5 |
| CaMKIdelta(h) | CAMK1D | Homo sapiens | -12.8 |
| CaMKIgamma(h) | CAMK1G | Homo sapiens | -0.4 |
| CaMKIIalpha(h) | CAMK2A | Homo sapiens | -6.9 |
| CaMKIIbeta(h) | CAMK2B | Homo sapiens | -0.3 |
| CaMKIIdelta(h) | CAMK2D | Homo sapiens | -13.5 |
| CaMKIIgamma(h) | CAMK2G | Homo sapiens | -3.0 |
| CaMKIV(h) | CAMK4 | Homo sapiens | 10.4 |
| CaMKK1(h) | CAMKK1 | Homo sapiens | -5.0 |
| CaMKK2(h) | CAMKK2 | Homo sapiens | -6.9 |
| Cdc7/cyclinB1(h) |
CDC7 CCNB1 |
Homo sapiens | 9.8 |
| CDK1/cyclinB(h) |
CDK1 CCNB1 CCNB2 |
Homo sapiens | -5.4 |
| CDK14/cyclinY(h) |
CDK14 CCNY |
Homo sapiens | -0.6 |
| CDK16/cyclinY(h) |
CDK16 CCNY |
Homo sapiens | -5.4 |
| CDK17/cyclinY(h) |
CDK17 CCNY |
Homo sapiens | 5.5 |
| CDK18/cyclinY(h) |
CDK18 CCNY |
Homo sapiens | 2.3 |
| CDK2/cyclinA(h) |
CDK2 CCNA2 |
Homo sapiens | -28.7 |
| CDK2/cyclinE(h) |
CDK2 CCNE1 |
Homo sapiens | 0.0 |
| CDK3/cyclinE(h) |
CDK3 CCNE1 |
Homo sapiens | -31.2 |
| CDK4/cyclinD3(h) |
CDK4 CCND3 |
Homo sapiens | 5.6 |
| CDK5/p25(h) |
CDK5 CDK5R1 |
Homo sapiens | -11.1 |
| CDK5/p35(h) |
CDK5 CDK5R1 |
Homo sapiens | -20.2 |
| CDK6/cyclinD3(h) |
CDK6 CCND3 |
Homo sapiens | -0.6 |
| CDK7/cyclinH/MAT1(h) |
CDK7 CCNH MNAT1 |
Homo sapiens | -11.9 |
| CDK9/cyclin T1(h) |
CDK9 CCNT1 |
Homo sapiens | -3.1 |
| CDKL1(h) | CDKL1 | Homo sapiens | 1.8 |
| CDKL2(h) | CDKL2 | Homo sapiens | -11.6 |
| CDKL3(h) | CDKL3 | Homo sapiens | 0.3 |
| CDKL4(h) | CDKL4 | Homo sapiens | 5.6 |
| ChaK1(h) | TRPM7 | Homo sapiens | -10.5 |
| CHK1(h) | CHEK1 | Homo sapiens | 2.4 |
| CHK2(h) | CHEK2 | Homo sapiens | -8.5 |
| CK1alpha(h) | CSNK1A1 | Homo sapiens | -1.7 |
| CK1delta(h) | CSNK1D | Homo sapiens | -3.1 |
| CK1epsilon(h) | CSNK1E | Homo sapiens | 1.3 |
| CK1gamma1(h) | CSNK1G1 | Homo sapiens | -11.3 |
| CK1gamma2(h) | CSNK1G2 | Homo sapiens | 4.6 |
| CK1gamma3(h) | CSNK1G3 | Homo sapiens | -8.8 |
| CK2(h) | Homo sapiens | 5.4 | |
| CK2alpha1(h) | CSNK2A1 | Homo sapiens | -17.5 |
| CK2alpha2(h) | CSNK2A2 | Homo sapiens | -3.5 |
| cKit(h) | KIT | Homo sapiens | 4.3 |
| CLIK1(h) | STK35 | Homo sapiens | 9.3 |
| CLK1(h) | CLK1 | Homo sapiens | 7.8 |
| CLK2(h) | CLK2 | Homo sapiens | -2.6 |
| CLK3(h) | CLK3 | Homo sapiens | -0.4 |
| CLK4(h) | CLK4 | Homo sapiens | 1.4 |
| COT(h) | MAP3K8 | Homo sapiens | -0.6 |
| c-RAF(h) | RAF1 | Homo sapiens | -1.5 |
| CRIK(h) | CIT | Homo sapiens | -10.7 |
| CSK(h) | CSK | Homo sapiens | -8.6 |
| cSRC(h) | SRC | Homo sapiens | -5.8 |
| DAPK1(h) | DAPK1 | Homo sapiens | -1.8 |
| DAPK2(h) | DAPK2 | Homo sapiens | -2.6 |
| DCAMKL1(h) | DCLK1 | Homo sapiens | -1.3 |
| DCAMKL2(h) | DCLK2 | Homo sapiens | -9.3 |
| DCAMKL3(h) | DCLK3 | Homo sapiens | -4.8 |
| DDR1(h) | DDR1 | Homo sapiens | 7.3 |
| DDR2(h) | DDR2 | Homo sapiens | -13.2 |
| DMPK(h) | DMPK | Homo sapiens | 12.7 |
| DRAK1(h) | STK17A | Homo sapiens | -9.6 |
| DRAK2(h) | STK17B | Homo sapiens | 2.4 |
| DYRK1A(h) | DYRK1A | Homo sapiens | 9.0 |
| DYRK1B(h) | DYRK1B | Homo sapiens | 15.8 |
| DYRK2(h) | DYRK2 | Homo sapiens | -0.8 |
| DYRK3(h) | DYRK3 | Homo sapiens | -1.8 |
| eEF-2K(h) | EEF2K | Homo sapiens | -9.4 |
| EGFR(h) | EGFR | Homo sapiens | -5.8 |
| EphA1(h) | EPHA1 | Homo sapiens | 7.7 |
| EphA2(h) | EPHA2 | Homo sapiens | -2.0 |
| EphA3(h) | EPHA3 | Homo sapiens | -7.5 |
| EphA4(h) | EPHA4 | Homo sapiens | -0.4 |
| EphA5(h) | EPHA5 | Homo sapiens | -3.7 |
| EphA7(h) | EPHA7 | Homo sapiens | 4.1 |
| EphA8(h) | EPHA8 | Homo sapiens | 4.6 |
| EphB1(h) | EPHB1 | Homo sapiens | 4.7 |
| EphB2(h) | EPHB2 | Homo sapiens | 6.9 |
| EphB3(h) | EPHB3 | Homo sapiens | 1.8 |
| EphB4(h) | EPHB4 | Homo sapiens | -19.1 |
| ErbB2(h) | ERBB2 | Homo sapiens | -6.4 |
| ErbB4(h) | ERBB4 | Homo sapiens | -4.4 |
| FAK(h) | PTK2 | Homo sapiens | -3.0 |
| Fer(h) | FER | Homo sapiens | -2.1 |
| Fes(h) | FES | Homo sapiens | -38.9 |
| FGFR1(h) | FGFR1 | Homo sapiens | 1.8 |
| FGFR2(h) | FGFR2 | Homo sapiens | -7.7 |
| FGFR3(h) | FGFR3 | Homo sapiens | -14.7 |
| FGFR4(h) | FGFR4 | Homo sapiens | -24.2 |
| Fgr(h) | FGR | Homo sapiens | -27.2 |
| Flt1(h) | FLT1 | Homo sapiens | -9.2 |
| Flt3(h) | FLT3 | Homo sapiens | 0.7 |
| Flt4(h) | FLT4 | Homo sapiens | 4.2 |
| Fms(h) | CSF1R | Homo sapiens | -2.5 |
| Fyn(h) | FYN | Homo sapiens | -1.8 |
| GAK(h) | GAK | Homo sapiens | 10.4 |
| GCK (h) | GCK | Homo sapiens | -4.7 |
| GCN2(h) | EIF2AK4 | Homo sapiens | 13.1 |
| GRK1(h) | GRK1 | Homo sapiens | 6.6 |
| GRK2(h) | GRK2 | Homo sapiens | 5.9 |
| GRK3(h) | GRK3 | Homo sapiens | 2.8 |
| GRK4(h) | GRK4 | Homo sapiens | -0.1 |
| GRK5(h) | GRK5 | Homo sapiens | 2.6 |
| GRK6(h) | GRK6 | Homo sapiens | 1.2 |
| GRK7(h) | GRK7 | Homo sapiens | 0.1 |
| GSK3alpha(h) | GSK3A | Homo sapiens | -11.4 |
| GSK3beta(h) | GSK3B | Homo sapiens | -4.2 |
| Haspin(h) | HASPIN | Homo sapiens | 2.1 |
| Hck(h) | HCK | Homo sapiens | -19.3 |
| Hck(h) activated | HCK | Homo sapiens | -4.0 |
| HIPK1(h) | HIPK1 | Homo sapiens | -2.9 |
| HIPK2(h) | HIPK2 | Homo sapiens | -6.3 |
| HIPK3(h) | HIPK3 | Homo sapiens | 3.3 |
| HIPK4(h) | HIPK4 | Homo sapiens | -3.6 |
| HPK1(h) | MAP4K1 | Homo sapiens | -13.0 |
| HRI(h) | EIF2AK1 | Homo sapiens | 6.6 |
| ICK(h) | CILK1 | Homo sapiens | -26.2 |
| IGF-1R(h) | IGF1R | Homo sapiens | -11.4 |
| IGF-1R(h), activated | IGF1R | Homo sapiens | -6.9 |
| IKKalpha(h) | CHUK | Homo sapiens | -24.9 |
| IKKbeta(h) | IKBKB | Homo sapiens | -20.2 |
| IKKepsilon(h) | IKBKE | Homo sapiens | 3.0 |
| IR(h) | INSR | Homo sapiens | -5.2 |
| IR(h), activated | INSR | Homo sapiens | -4.0 |
| IRAK1(h) | IRAK1 | Homo sapiens | -0.2 |
| IRAK4(h) | IRAK4 | Homo sapiens | 3.6 |
| IRE1(h) | ERN1 | Homo sapiens | 5.6 |
| IRR(h) | INSRR | Homo sapiens | 0.5 |
| Itk(h) | ITK | Homo sapiens | -7.2 |
| JAK1(h) | JAK1 | Homo sapiens | -1.7 |
| JAK2(h) | JAK2 | Homo sapiens | -22.0 |
| JAK3(h) | JAK3 | Homo sapiens | -1.9 |
| JNK1alpha1(h) | MAPK8 | Homo sapiens | -3.8 |
| JNK2alpha2(h) | MAPK9 | Homo sapiens | -1.7 |
| JNK3(h) | MAPK10 | Homo sapiens | 0.7 |
| KDR(h) | KDR | Homo sapiens | 1.3 |
| LATS1(h) | LATS1 | Homo sapiens | -5.4 |
| LATS2(h) | LATS2 | Homo sapiens | 3.2 |
| Lck(h) | LCK | Homo sapiens | -14.4 |
| Lck(h) activated | LCK | Homo sapiens | -0.2 |
| LIMK1(h) | LIMK1 | Homo sapiens | 0.6 |
| LIMK2(h) | LIMK2 | Homo sapiens | 0.3 |
| LKB1(h) | STK11 | Homo sapiens | -1.5 |
| LOK(h) | STK10 | Homo sapiens | 2.5 |
| LRRK2(h) | LRRK2 | Homo sapiens | 5.1 |
| LTK(h) | LTK | Homo sapiens | 4.2 |
| Lyn(h) | LYN | Homo sapiens | -5.9 |
| MAK(h) | MAK | Homo sapiens | 5.1 |
| MAP4K3(h) | MAP4K3 | Homo sapiens | -14.8 |
| MAP4K4(h) | MAP4K4 | Homo sapiens | -1.5 |
| MAP4K5(h) | MAP4K5 | Homo sapiens | 6.2 |
| MAPK1(h) | MAPK1 | Homo sapiens | 7.3 |
| MAPK2(h) | Homo sapiens | 11.1 | |
| MAPKAP-K2(h) | MAPKAPK2 | Homo sapiens | -21.4 |
| MAPKAP-K3(h) | MAPKAPK3 | Homo sapiens | -7.0 |
| MARK1(h) | MARK1 | Homo sapiens | 0.1 |
| MARK3(h) | MARK3 | Homo sapiens | -2.1 |
| MARK4(h) | MARK4 | Homo sapiens | 2.7 |
| MATK(h) | MATK | Homo sapiens | 0.8 |
| MEK1(h) | MAP2K1 | Homo sapiens | -3.7 |
| MEK2(h) | MAP2K2 | Homo sapiens | 0.3 |
| MEKK2(h) | MAP3K2 | Homo sapiens | 7.5 |
| MEKK3(h) | MAP3K3 | Homo sapiens | 2.3 |
| MELK(h) | MELK | Homo sapiens | 10.8 |
| Mer(h) | MERTK | Homo sapiens | -0.9 |
| Met(h) | MET | Homo sapiens | -15.8 |
| MINK(h) | MINK1 | Homo sapiens | 5.2 |
| MKK3(h) | MAP2K3 | Homo sapiens | -0.6 |
| MKK6(h) | MAP2K6 | Homo sapiens | 7.3 |
| MLCK(h) | MYLK3 | Homo sapiens | 1.7 |
| MLK1(h) | MAP3K9 | Homo sapiens | 3.5 |
| MLK2(h) | MAP3K10 | Homo sapiens | 4.2 |
| MLK3(h) | MAP3K11 | Homo sapiens | 11.4 |
| MLK4(h) | MAP3K21 | Homo sapiens | 6.1 |
| Mnk1(h) | MKNK1 | Homo sapiens | -27.5 |
| Mnk2(h) | MKNK2 | Homo sapiens | 3.5 |
| MOK(h) | MOK | Homo sapiens | -23.2 |
| MRCKalpha(h) | CDC42BPA | Homo sapiens | -2.4 |
| MRCKbeta(h) | CDC42BPB | Homo sapiens | -2.2 |
| MRCKgamma(h) | CDC42BPG | Homo sapiens | 2.1 |
| MSK1(h) | RPS6KA5 | Homo sapiens | -5.9 |
| MSK2(h) | RPS6KA4 | Homo sapiens | -20.8 |
| MSSK1(h) | SRPK3 | Homo sapiens | -10.0 |
| MST1(h) | STK4 | Homo sapiens | 9.3 |
| MST2(h) | STK3 | Homo sapiens | -2.8 |
| MST3(h) | STK24 | Homo sapiens | 3.0 |
| MST4(h) | STK26 | Homo sapiens | -2.7 |
| mTOR FKBP12(h) |
MTOR FKBP1A |
Homo sapiens | 2.5 |
| mTOR(h) | MTOR | Homo sapiens | -1.5 |
| MuSK(h) | MUSK | Homo sapiens | -2.4 |
| MYLK2(h) | MYLK2 | Homo sapiens | 3.0 |
| MYO3B(h) | MYO3B | Homo sapiens | 2.5 |
| NDR1(h) | STK38 | Homo sapiens | -4.7 |
| NDR2(h) | STK38L | Homo sapiens | -15.7 |
| NEK1(h) | NEK1 | Homo sapiens | -11.9 |
| NEK11(h) | NEK11 | Homo sapiens | 16.2 |
| NEK2(h) | NEK2 | Homo sapiens | 3.2 |
| NEK3(h) | NEK3 | Homo sapiens | 61.0 |
| NEK4(h) | NEK4 | Homo sapiens | 13.1 |
| NEK5(h) | NEK5 | Homo sapiens | 6.2 |
| NEK6(h) | NEK6 | Homo sapiens | 4.9 |
| NEK7(h) | NEK7 | Homo sapiens | 3.8 |
| NEK9(h) | NEK9 | Homo sapiens | 7.9 |
| NIM1(h) | NIM1K | Homo sapiens | 5.8 |
| NLK (h) | NLK | Homo sapiens | -2.5 |
| NUAK2(h) | NUAK2 | Homo sapiens | 5.0 |
| OSR1(h) | OXSR1 | Homo sapiens | -23.5 |
| p70S6K(h) | Homo sapiens | 1.0 | |
| p70S6Kbeta(h) | RPS6KB1 | Homo sapiens | 1.9 |
| PAK1(h) | PAK1 | Homo sapiens | 5.2 |
| PAK2(h) | PAK2 | Homo sapiens | 3.1 |
| PAK3(h) | PAK3 | Homo sapiens | 1.7 |
| PAK4(h) | PAK4 | Homo sapiens | -1.8 |
| PAK5(h) | PAK5 | Homo sapiens | -3.6 |
| PAK6(h) | PAK6 | Homo sapiens | -4.8 |
| PAR-1Balpha(h) | MARK2 | Homo sapiens | 7.5 |
| PASK(h) | PASK | Homo sapiens | -5.0 |
| PDGFRalpha(h) | PDGFRA | Homo sapiens | -17.2 |
| PDGFRbeta(h) | PDGFRB | Homo sapiens | -5.2 |
| PDHK2(h) | PDK2 | Homo sapiens | -14.1 |
| PDHK4(h) | PDK4 | Homo sapiens | 9.0 |
| PDK1(h) | PDK1 | Homo sapiens | -3.6 |
| PEK(h) | EIF2AK3 | Homo sapiens | 1.8 |
| PhKgamma1(h) | PHKG1 | Homo sapiens | -1.6 |
| PhKgamma2(h) | PHKG2 | Homo sapiens | 0.7 |
| Pim-1(h) | PIM1 | Homo sapiens | 1.0 |
| Pim-2(h) | PIM2 | Homo sapiens | -3.0 |
| Pim-3(h) | PIM3 | Homo sapiens | 3.1 |
| PKA(h) | Homo sapiens | -3.5 | |
| PKACbeta(h) | PRKACB | Homo sapiens | -5.1 |
| PKBalpha(h) | AKT1 | Homo sapiens | -3.9 |
| PKBbeta(h) | AKT2 | Homo sapiens | -27.9 |
| PKBgamma(h) | AKT3 | Homo sapiens | -6.7 |
| PKCalpha(h) | PRKCA | Homo sapiens | 1.1 |
| PKCbetaI(h) | PRKCB | Homo sapiens | 2.8 |
| PKCbetaII(h) | PRKCB | Homo sapiens | 2.9 |
| PKCdelta(h) | PRKCD | Homo sapiens | 2.1 |
| PKCepsilon(h) | PRKCE | Homo sapiens | 19.1 |
| PKCeta(h) | PRKCH | Homo sapiens | 4.4 |
| PKCgamma(h) | PRKCG | Homo sapiens | 3.2 |
| PKCiota(h) | PRKCI | Homo sapiens | -3.9 |
| PKCmu(h) | PRKD1 | Homo sapiens | -6.5 |
| PKCtheta(h) | PRKCQ | Homo sapiens | 3.4 |
| PKCzeta(h) | PRKCZ | Homo sapiens | 18.7 |
| PKD2(h) | PRKD2 | Homo sapiens | 1.6 |
| PKD3(h) | PRKD3 | Homo sapiens | -0.8 |
| PKG1alpha(h) | PRKG1 | Homo sapiens | -5.4 |
| PKG1beta(h) | PRKG1 | Homo sapiens | 1.8 |
| PKR(h) | EIF2AK2 | Homo sapiens | 1.3 |
| Plk1(h) | PLK1 | Homo sapiens | -2.9 |
| Plk3(h) | PLK3 | Homo sapiens | 0.5 |
| Plk4(h) | PLK4 | Homo sapiens | -5.7 |
| PRAK(h) | MAPKAPK5 | Homo sapiens | 11.5 |
| PRK1(h) | PKN1 | Homo sapiens | -3.9 |
| PRK2(h) | PKN2 | Homo sapiens | 7.5 |
| PRKG2(h) | PRKG2 | Homo sapiens | -2.9 |
| PrKX(h) | PRKX | Homo sapiens | 1.4 |
| PRP4(h) | PRPF4B | Homo sapiens | 6.8 |
| PTK5(h) | FRK | Homo sapiens | 0.3 |
| Pyk2(h) | PTK2B | Homo sapiens | -2.0 |
| Ret(h) | RET | Homo sapiens | -9.4 |
| RIPK1(h) | RIPK1 | Homo sapiens | 0.7 |
| RIPK2(h) | RIPK2 | Homo sapiens | -1.0 |
| ROCK-I(h) | ROCK1 | Homo sapiens | -2.7 |
| ROCK-II(h) | ROCK2 | Homo sapiens | 18.1 |
| Ron(h) | MST1R | Homo sapiens | -9.4 |
| Ros(h) | ROS1 | Homo sapiens | -1.0 |
| Rse(h) | TYRO3 | Homo sapiens | -20.3 |
| Rsk1(h) | RPS6KA1 | Homo sapiens | -23.6 |
| Rsk2(h) | RPS6KA3 | Homo sapiens | -14.9 |
| Rsk3(h) | RPS6KA2 | Homo sapiens | 9.7 |
| Rsk4(h) | RPS6KA6 | Homo sapiens | -40.5 |
| SAPK2a(h) | MAPK14 | Homo sapiens | -8.6 |
| SAPK2b(h) | MAPK11 | Homo sapiens | 1.3 |
| SAPK3(h) | MAPK12 | Homo sapiens | -0.1 |
| SAPK4(h) | MAPK13 | Homo sapiens | -3.8 |
| SBK1(h) | SBK1 | Homo sapiens | -2.6 |
| SGK(h) | SGK1 | Homo sapiens | -18.0 |
| SGK2(h) | SGK2 | Homo sapiens | -17.6 |
| SGK3(h) | SGK3 | Homo sapiens | -6.1 |
| SIK(h) | SIK1 | Homo sapiens | -39.0 |
| SIK2(h) | SIK2 | Homo sapiens | -3.1 |
| SIK3(h) | SIK3 | Homo sapiens | -19.3 |
| SLK(h) | SLK | Homo sapiens | -14.4 |
| Snk(h) | PLK2 | Homo sapiens | -4.5 |
| SNRK(h) | SNRK | Homo sapiens | -22.1 |
| SRMS(h) | SRMS | Homo sapiens | 7.1 |
| SRPK1(h) | SRPK1 | Homo sapiens | -6.8 |
| SRPK2(h) | SRPK2 | Homo sapiens | -4.8 |
| STK16(h) | STK16 | Homo sapiens | 4.1 |
| STK25(h) | STK25 | Homo sapiens | 9.0 |
| STK32A(h) | STK32A | Homo sapiens | 3.2 |
| STK32B(h) | STK32B | Homo sapiens | -1.0 |
| STK32C(h) | STK32C | Homo sapiens | 1.1 |
| STK33(h) | STK33 | Homo sapiens | 6.4 |
| STK39(h) | STK39 | Homo sapiens | -27.2 |
| Syk(h) | SYK | Homo sapiens | -8.6 |
| TAF1L(h) | TAF1L | Homo sapiens | 2.8 |
| TAK1(h) | MAP3K7 | Homo sapiens | -6.4 |
| TAO1(h) | TAOK1 | Homo sapiens | 2.7 |
| TAO2(h) | TAOK2 | Homo sapiens | -4.1 |
| TAO3(h) | TAOK3 | Homo sapiens | 5.6 |
| TBK1(h) | TBK1 | Homo sapiens | -3.0 |
| Tec(h) activated | TEC | Homo sapiens | -7.4 |
| TGFBR1(h) | TGFBR1 | Homo sapiens | 5.1 |
| TGFBR2(h) | TGFBR2 | Homo sapiens | 8.9 |
| Tie2(h) | TEK | Homo sapiens | -8.2 |
| TLK1(h) | TLK1 | Homo sapiens | -3.1 |
| TLK2(h) | TLK2 | Homo sapiens | -5.5 |
| TNIK(h) | TNIK | Homo sapiens | -32.9 |
| TRB2(h) | TRIB2 | Homo sapiens | -2.4 |
| TrkA(h) | NTRK1 | Homo sapiens | -12.2 |
| TrkB(h) | NTRK2 | Homo sapiens | -11.7 |
| TrkC(h) | NTRK3 | Homo sapiens | -6.4 |
| TSSK1(h) | TSSK1B | Homo sapiens | -5.6 |
| TSSK2(h) | TSSK2 | Homo sapiens | -2.0 |
| TSSK3(h) | TSSK3 | Homo sapiens | -7.5 |
| TSSK4(h) | TSSK4 | Homo sapiens | -14.6 |
| TTBK1(h) | TTBK1 | Homo sapiens | -7.8 |
| TTBK2(h) | TTBK2 | Homo sapiens | -8.6 |
| TTK(h) | TTK | Homo sapiens | 2.1 |
| Txk(h) | TXK | Homo sapiens | -27.0 |
| TYK2(h) | TYK2 | Homo sapiens | 8.8 |
| ULK1(h) | ULK1 | Homo sapiens | -12.6 |
| ULK2(h) | ULK2 | Homo sapiens | 5.1 |
| ULK3(h) | ULK3 | Homo sapiens | 10.9 |
| VRK1(h) | VRK1 | Homo sapiens | 12.3 |
| VRK2(h) | VRK2 | Homo sapiens | 6.6 |
| WEE1(h) | WEE1 | Homo sapiens | -11.9 |
| Wee1B(h) | WEE2 | Homo sapiens | 7.5 |
| WNK1(h) | WNK1 | Homo sapiens | 6.4 |
| WNK2(h) | WNK2 | Homo sapiens | -15.2 |
| WNK3(h) | WNK3 | Homo sapiens | -3.4 |
| WNK4(h) | WNK4 | Homo sapiens | 10.5 |
| Yes(h) | YES1 | Homo sapiens | -6.9 |
| ZAK(h) | MAP3K20 | Homo sapiens | -4.9 |
| ZAP-70(h) | ZAP70 | Homo sapiens | 2.7 |
| ZIPK(h) | DAPK3 | Homo sapiens | -5.1 |
| ATM(h) | ATM | Homo sapiens | 2.0 |
| ATR/ATRIP(h) |
ATR ATRIP |
Homo sapiens | -5.3 |
| DNA-PK(h) | PRKDC | Homo sapiens | -4.2 |
| PI3 Kinase (p110a/p85a)(h) |
PIK3CA PIK3R1 |
Homo sapiens | -2.9 |
| PI3 Kinase (p110b/p85a)(h) |
PIK3CB PIK3R1 |
Homo sapiens | -2.0 |
| PI3 Kinase (p110d/p85a)(h) |
PIK3CD PIK3R1 |
Homo sapiens | -1.4 |
| PI3 Kinase (p120g)(h) | PIK3CG | Homo sapiens | 14.1 |
| PI3KC2a(h) | PIK3C2A | Homo sapiens | 11.6 |
| PI3KC2g(h) | PIK3C2G | Homo sapiens | 6.4 |
| PIP4K2a(h) | PIP4K2A | Homo sapiens | -0.8 |
| PIP5K1a(h) | PIP5K1A | Homo sapiens | -9.1 |
| PIP5K1g(h) | PIP5K1C | Homo sapiens | -2.1 |
BAY-2297
Conclusion: Closest off-target is PIK3C2A (27.49 % inhibition).
| Target protein | HGNC name | Species | % inhibition at 10 µM |
|---|---|---|---|
| AAK1(h) | AAK1 | Homo sapiens | -10.2 |
| Abl(h) | ABL1 | Homo sapiens | -3.6 |
| ACK1(h) | TNK2 | Homo sapiens | 8.4 |
| ACTR2(h) | ACTR2 | Homo sapiens | 6.3 |
| ALK(h) | ALK | Homo sapiens | -8.9 |
| ALK1(h) | ACVRL1 | Homo sapiens | -1.3 |
| ALK2(h) | ACVR1 | Homo sapiens | -2.3 |
| ALK4(h) | ACVR1B | Homo sapiens | 3.0 |
| ALK6(h) | BMPR1B | Homo sapiens | -1.0 |
| AMPKalpha1(h) | PRKAA1 | Homo sapiens | -6.7 |
| AMPKalpha2(h) | PRKAA2 | Homo sapiens | -2.8 |
| A-Raf(h) | ARAF | Homo sapiens | 2.6 |
| Arg(h) | ABL2 | Homo sapiens | 2.0 |
| ARK5(h) | NUAK1 | Homo sapiens | -2.4 |
| ASK1(h) | MAP3K5 | Homo sapiens | -1.5 |
| Aurora-A(h) | AURKA | Homo sapiens | 12.7 |
| Aurora-B(h) | AURKB | Homo sapiens | -17.8 |
| Aurora-C(h) | AURKC | Homo sapiens | -11.4 |
| Axl(h) | AXL | Homo sapiens | 3.2 |
| BIKe(h) | BMP2K | Homo sapiens | -1.6 |
| Blk(h) | BLK | Homo sapiens | -14.4 |
| BMPR2(h) | BMPR2 | Homo sapiens | 14.4 |
| Bmx(h) | BMX | Homo sapiens | -7.7 |
| B-Raf(h) | BRAF | Homo sapiens | -3.0 |
| BRK(h) | PTK6 | Homo sapiens | -8.0 |
| BrSK1(h) | BRSK1 | Homo sapiens | 5.0 |
| BrSK2(h) | BRSK2 | Homo sapiens | -10.1 |
| BTK(h) | BTK | Homo sapiens | -10.5 |
| CaMKI(h) | CAMK1 | Homo sapiens | -5.0 |
| CaMKIbeta(h) | PNCK | Homo sapiens | -9.0 |
| CaMKIdelta(h) | CAMK1D | Homo sapiens | -12.8 |
| CaMKIgamma(h) | CAMK1G | Homo sapiens | 0.7 |
| CaMKIIalpha(h) | CAMK2A | Homo sapiens | -13.1 |
| CaMKIIbeta(h) | CAMK2B | Homo sapiens | -8.6 |
| CaMKIIdelta(h) | CAMK2D | Homo sapiens | -4.4 |
| CaMKIIgamma(h) | CAMK2G | Homo sapiens | 0.3 |
| CaMKIV(h) | CAMK4 | Homo sapiens | 8.3 |
| CaMKK1(h) | CAMKK1 | Homo sapiens | 1.2 |
| CaMKK2(h) | CAMKK2 | Homo sapiens | -6.7 |
| Cdc7/cyclinB1(h) | CDC7,CCNB1 | Homo sapiens | 3.7 |
| CDK1/cyclinB(h) | CDK1,CCNB1,CCNB2 | Homo sapiens | -8.5 |
| CDK14/cyclinY(h) | CDK14,CCNY | Homo sapiens | -0.2 |
| CDK16/cyclinY(h) | CDK16,CCNY | Homo sapiens | 4.6 |
| CDK17/cyclinY(h) | CDK17,CCNY | Homo sapiens | 3.8 |
| CDK18/cyclinY(h) | CDK18,CCNY | Homo sapiens | -1.8 |
| CDK2/cyclinA(h) | CDK2,CCNA2 | Homo sapiens | -22.1 |
| CDK2/cyclinE(h) | CDK2,CCNE1 | Homo sapiens | 3.4 |
| CDK3/cyclinE(h) | CDK3,CCNE1 | Homo sapiens | -27.9 |
| CDK4/cyclinD3(h) | CDK4,CCND3 | Homo sapiens | 7.5 |
| CDK5/p25(h) | CDK5,CDK5R1 | Homo sapiens | 2.1 |
| CDK5/p35(h) | CDK5,CDK5R1 | Homo sapiens | -12.5 |
| CDK6/cyclinD3(h) | CDK6,CCND3 | Homo sapiens | 0.3 |
| CDK7/cyclinH/MAT1(h) | CDK7,CCNH,MNAT1 | Homo sapiens | -14.6 |
| CDK9/cyclin T1(h) | CDK9,CCNT1 | Homo sapiens | -1.8 |
| CDKL1(h) | CDKL1 | Homo sapiens | 6.3 |
| CDKL2(h) | CDKL2 | Homo sapiens | -7.4 |
| CDKL3(h) | CDKL3 | Homo sapiens | -5.9 |
| CDKL4(h) | CDKL4 | Homo sapiens | -1.9 |
| ChaK1(h) | TRPM7 | Homo sapiens | 0.0 |
| CHK1(h) | CHEK1 | Homo sapiens | 1.7 |
| CHK2(h) | CHEK2 | Homo sapiens | -17.7 |
| CK1alpha(h) | CSNK1A1 | Homo sapiens | -1.1 |
| CK1delta(h) | CSNK1D | Homo sapiens | -5.2 |
| CK1epsilon(h) | CSNK1E | Homo sapiens | 4.5 |
| CK1gamma1(h) | CSNK1G1 | Homo sapiens | -19.7 |
| CK1gamma2(h) | CSNK1G2 | Homo sapiens | -1.3 |
| CK1gamma3(h) | CSNK1G3 | Homo sapiens | -8.5 |
| CK2(h) | Homo sapiens | -3.4 | |
| CK2alpha1(h) | CSNK2A1 | Homo sapiens | -26.4 |
| CK2alpha2(h) | CSNK2A2 | Homo sapiens | 6.4 |
| cKit(h) | KIT | Homo sapiens | 7.7 |
| CLIK1(h) | STK35 | Homo sapiens | 7.3 |
| CLK1(h) | CLK1 | Homo sapiens | 7.1 |
| CLK2(h) | CLK2 | Homo sapiens | -2.2 |
| CLK3(h) | CLK3 | Homo sapiens | 1.4 |
| CLK4(h) | CLK4 | Homo sapiens | -12.4 |
| COT(h) | MAP3K8 | Homo sapiens | -1.4 |
| c-RAF(h) | RAF1 | Homo sapiens | -1.5 |
| CRIK(h) | CIT | Homo sapiens | -2.1 |
| CSK(h) | CSK | Homo sapiens | -8.5 |
| cSRC(h) | SRC | Homo sapiens | 0.9 |
| DAPK1(h) | DAPK1 | Homo sapiens | -5.7 |
| DAPK2(h) | DAPK2 | Homo sapiens | 11.7 |
| DCAMKL1(h) | DCLK1 | Homo sapiens | -2.6 |
| DCAMKL2(h) | DCLK2 | Homo sapiens | -8.5 |
| DCAMKL3(h) | DCLK3 | Homo sapiens | -6.1 |
| DDR1(h) | DDR1 | Homo sapiens | 0.9 |
| DDR2(h) | DDR2 | Homo sapiens | -10.2 |
| DMPK(h) | DMPK | Homo sapiens | 4.5 |
| DRAK1(h) | STK17A | Homo sapiens | -1.4 |
| DRAK2(h) | STK17B | Homo sapiens | -2.6 |
| DYRK1A(h) | DYRK1A | Homo sapiens | 3.5 |
| DYRK1B(h) | DYRK1B | Homo sapiens | 15.4 |
| DYRK2(h) | DYRK2 | Homo sapiens | -8.9 |
| DYRK3(h) | DYRK3 | Homo sapiens | -6.3 |
| eEF-2K(h) | EEF2K | Homo sapiens | -4.9 |
| EGFR(h) | EGFR | Homo sapiens | -4.7 |
| EphA1(h) | EPHA1 | Homo sapiens | 2.9 |
| EphA2(h) | EPHA2 | Homo sapiens | -5.2 |
| EphA3(h) | EPHA3 | Homo sapiens | 1.3 |
| EphA4(h) | EPHA4 | Homo sapiens | 0.2 |
| EphA5(h) | EPHA5 | Homo sapiens | -7.8 |
| EphA7(h) | EPHA7 | Homo sapiens | 3.4 |
| EphA8(h) | EPHA8 | Homo sapiens | 3.7 |
| EphB1(h) | EPHB1 | Homo sapiens | 9.8 |
| EphB2(h) | EPHB2 | Homo sapiens | -4.8 |
| EphB3(h) | EPHB3 | Homo sapiens | 7.4 |
| EphB4(h) | EPHB4 | Homo sapiens | -2.2 |
| ErbB2(h) | ERBB2 | Homo sapiens | -4.3 |
| ErbB4(h) | ERBB4 | Homo sapiens | -8.7 |
| FAK(h) | PTK2 | Homo sapiens | -5.4 |
| Fer(h) | FER | Homo sapiens | -11.2 |
| Fes(h) | FES | Homo sapiens | -7.8 |
| FGFR1(h) | FGFR1 | Homo sapiens | -0.1 |
| FGFR2(h) | FGFR2 | Homo sapiens | -6.4 |
| FGFR3(h) | FGFR3 | Homo sapiens | -0.4 |
| FGFR4(h) | FGFR4 | Homo sapiens | -8.4 |
| Fgr(h) | FGR | Homo sapiens | -7.1 |
| Flt1(h) | FLT1 | Homo sapiens | -11.4 |
| Flt3(h) | FLT3 | Homo sapiens | -4.6 |
| Flt4(h) | FLT4 | Homo sapiens | 11.3 |
| Fms(h) | CSF1R | Homo sapiens | 5.3 |
| Fyn(h) | FYN | Homo sapiens | 5.5 |
| GAK(h) | GAK | Homo sapiens | 0.3 |
| GCK (h) | GCK | Homo sapiens | -20.7 |
| GCN2(h) | EIF2AK4 | Homo sapiens | 12.4 |
| GRK1(h) | GRK1 | Homo sapiens | -8.5 |
| GRK2(h) | GRK2 | Homo sapiens | -6.2 |
| GRK3(h) | GRK3 | Homo sapiens | -3.1 |
| GRK4(h) | GRK4 | Homo sapiens | -1.5 |
| GRK5(h) | GRK5 | Homo sapiens | -0.6 |
| GRK6(h) | GRK6 | Homo sapiens | -0.2 |
| GRK7(h) | GRK7 | Homo sapiens | -3.6 |
| GSK3alpha(h) | GSK3A | Homo sapiens | -1.7 |
| GSK3beta(h) | GSK3B | Homo sapiens | -10.3 |
| Haspin(h) | HASPIN | Homo sapiens | -2.8 |
| Hck(h) | HCK | Homo sapiens | -12.9 |
| Hck(h) activated | HCK | Homo sapiens | -9.4 |
| HIPK1(h) | HIPK1 | Homo sapiens | 1.3 |
| HIPK2(h) | HIPK2 | Homo sapiens | -9.4 |
| HIPK3(h) | HIPK3 | Homo sapiens | 2.6 |
| HIPK4(h) | HIPK4 | Homo sapiens | 4.6 |
| HPK1(h) | MAP4K1 | Homo sapiens | -12.5 |
| HRI(h) | EIF2AK1 | Homo sapiens | -5.1 |
| ICK(h) | CILK1 | Homo sapiens | -9.8 |
| IGF-1R(h) | IGF1R | Homo sapiens | -8.9 |
| IGF-1R(h), activated | IGF1R | Homo sapiens | -4.3 |
| IKKalpha(h) | CHUK | Homo sapiens | -2.7 |
| IKKbeta(h) | IKBKB | Homo sapiens | -16.6 |
| IKKepsilon(h) | IKBKE | Homo sapiens | 0.0 |
| IR(h) | INSR | Homo sapiens | -7.3 |
| IR(h), activated | INSR | Homo sapiens | 2.2 |
| IRAK1(h) | IRAK1 | Homo sapiens | 1.2 |
| IRAK4(h) | IRAK4 | Homo sapiens | -1.3 |
| IRE1(h) | ERN1 | Homo sapiens | 19.3 |
| IRR(h) | INSRR | Homo sapiens | -9.9 |
| Itk(h) | ITK | Homo sapiens | -2.7 |
| JAK1(h) | JAK1 | Homo sapiens | 8.7 |
| JAK2(h) | JAK2 | Homo sapiens | -5.0 |
| JAK3(h) | JAK3 | Homo sapiens | 2.8 |
| JNK1alpha1(h) | MAPK8 | Homo sapiens | -1.2 |
| JNK2alpha2(h) | MAPK9 | Homo sapiens | 2.3 |
| JNK3(h) | MAPK10 | Homo sapiens | 13.2 |
| KDR(h) | KDR | Homo sapiens | -2.8 |
| LATS1(h) | LATS1 | Homo sapiens | -2.7 |
| LATS2(h) | LATS2 | Homo sapiens | 5.1 |
| Lck(h) | LCK | Homo sapiens | -7.9 |
| Lck(h) activated | LCK | Homo sapiens | 2.1 |
| LIMK1(h) | LIMK1 | Homo sapiens | 0.4 |
| LIMK2(h) | LIMK2 | Homo sapiens | 1.5 |
| LKB1(h) | STK11 | Homo sapiens | 1.9 |
| LOK(h) | STK10 | Homo sapiens | 10.4 |
| LRRK2(h) | LRRK2 | Homo sapiens | 10.4 |
| LTK(h) | LTK | Homo sapiens | 5.8 |
| Lyn(h) | LYN | Homo sapiens | -1.9 |
| MAK(h) | MAK | Homo sapiens | 4.0 |
| MAP4K3(h) | MAP4K3 | Homo sapiens | -14.3 |
| MAP4K4(h) | MAP4K4 | Homo sapiens | 5.6 |
| MAP4K5(h) | MAP4K5 | Homo sapiens | -1.8 |
| MAPK1(h) | MAPK1 | Homo sapiens | -0.8 |
| MAPK2(h) | Homo sapiens | 11.3 | |
| MAPKAP-K2(h) | MAPKAPK2 | Homo sapiens | -16.7 |
| MAPKAP-K3(h) | MAPKAPK3 | Homo sapiens | -3.8 |
| MARK1(h) | MARK1 | Homo sapiens | 2.6 |
| MARK3(h) | MARK3 | Homo sapiens | -3.6 |
| MARK4(h) | MARK4 | Homo sapiens | 2.6 |
| MATK(h) | MATK | Homo sapiens | 4.2 |
| MEK1(h) | MAP2K1 | Homo sapiens | 4.6 |
| MEK2(h) | MAP2K2 | Homo sapiens | 6.8 |
| MEKK2(h) | MAP3K2 | Homo sapiens | 9.5 |
| MEKK3(h) | MAP3K3 | Homo sapiens | 7.5 |
| MELK(h) | MELK | Homo sapiens | 9.0 |
| Mer(h) | MERTK | Homo sapiens | -6.1 |
| Met(h) | MET | Homo sapiens | -3.8 |
| MINK(h) | MINK1 | Homo sapiens | 5.6 |
| MKK3(h) | MAP2K3 | Homo sapiens | -0.4 |
| MKK6(h) | MAP2K6 | Homo sapiens | 5.8 |
| MLCK(h) | MYLK3 | Homo sapiens | 1.7 |
| MLK1(h) | MAP3K9 | Homo sapiens | -1.3 |
| MLK2(h) | MAP3K10 | Homo sapiens | 0.4 |
| MLK3(h) | MAP3K11 | Homo sapiens | 14.9 |
| MLK4(h) | MAP3K21 | Homo sapiens | 8.5 |
| Mnk1(h) | MKNK1 | Homo sapiens | -9.9 |
| Mnk2(h) | MKNK2 | Homo sapiens | -0.8 |
| MOK(h) | MOK | Homo sapiens | -20.3 |
| MRCKalpha(h) | CDC42BPA | Homo sapiens | -5.0 |
| MRCKbeta(h) | CDC42BPB | Homo sapiens | -6.3 |
| MRCKgamma(h) | CDC42BPG | Homo sapiens | 1.1 |
| MSK1(h) | RPS6KA5 | Homo sapiens | -0.5 |
| MSK2(h) | RPS6KA4 | Homo sapiens | -22.2 |
| MSSK1(h) | SRPK3 | Homo sapiens | 9.3 |
| MST1(h) | STK4 | Homo sapiens | 2.5 |
| MST2(h) | STK3 | Homo sapiens | -1.5 |
| MST3(h) | STK24 | Homo sapiens | 5.6 |
| MST4(h) | STK26 | Homo sapiens | -4.7 |
| mTOR FKBP12(h) | MTOR,FKBP1A | Homo sapiens | -11.1 |
| mTOR(h) | MTOR | Homo sapiens | 5.3 |
| MuSK(h) | MUSK | Homo sapiens | 0.2 |
| MYLK2(h) | MYLK2 | Homo sapiens | 3.5 |
| MYO3B(h) | MYO3B | Homo sapiens | 6.9 |
| NDR1(h) | STK38 | Homo sapiens | -3.0 |
| NDR2(h) | STK38L | Homo sapiens | -23.7 |
| NEK1(h) | NEK1 | Homo sapiens | 5.5 |
| NEK11(h) | NEK11 | Homo sapiens | 15.8 |
| NEK2(h) | NEK2 | Homo sapiens | -1.1 |
| NEK3(h) | NEK3 | Homo sapiens | 5.4 |
| NEK4(h) | NEK4 | Homo sapiens | -10.2 |
| NEK5(h) | NEK5 | Homo sapiens | 8.7 |
| NEK6(h) | NEK6 | Homo sapiens | 5.3 |
| NEK7(h) | NEK7 | Homo sapiens | 1.5 |
| NEK9(h) | NEK9 | Homo sapiens | 9.4 |
| NIM1(h) | NIM1K | Homo sapiens | 3.0 |
| NLK (h) | NLK | Homo sapiens | -1.7 |
| NUAK2(h) | NUAK2 | Homo sapiens | -1.0 |
| OSR1(h) | OXSR1 | Homo sapiens | -18.7 |
| p70S6K(h) | Homo sapiens | 4.8 | |
| p70S6Kbeta(h) | RPS6KB1 | Homo sapiens | 3.7 |
| PAK1(h) | PAK1 | Homo sapiens | 5.2 |
| PAK2(h) | PAK2 | Homo sapiens | 2.0 |
| PAK3(h) | PAK3 | Homo sapiens | 7.3 |
| PAK4(h) | PAK4 | Homo sapiens | -2.4 |
| PAK5(h) | PAK5 | Homo sapiens | 1.5 |
| PAK6(h) | PAK6 | Homo sapiens | -5.8 |
| PAR-1Balpha(h) | MARK2 | Homo sapiens | 5.5 |
| PASK(h) | PASK | Homo sapiens | -0.4 |
| PDGFRalpha(h) | PDGFRA | Homo sapiens | -5.3 |
| PDGFRbeta(h) | PDGFRB | Homo sapiens | -9.1 |
| PDHK2(h) | PDK2 | Homo sapiens | -4.9 |
| PDHK4(h) | PDK4 | Homo sapiens | 5.7 |
| PDK1(h) | PDK1 | Homo sapiens | -8.4 |
| PEK(h) | EIF2AK3 | Homo sapiens | -1.5 |
| PhKgamma1(h) | PHKG1 | Homo sapiens | 7.2 |
| PhKgamma2(h) | PHKG2 | Homo sapiens | -3.5 |
| Pim-1(h) | PIM1 | Homo sapiens | 6.1 |
| Pim-2(h) | PIM2 | Homo sapiens | 4.9 |
| Pim-3(h) | PIM3 | Homo sapiens | 4.9 |
| PKA(h) | Homo sapiens | 2.6 | |
| PKACbeta(h) | PRKACB | Homo sapiens | -10.7 |
| PKBalpha(h) | AKT1 | Homo sapiens | -10.2 |
| PKBbeta(h) | AKT2 | Homo sapiens | -3.3 |
| PKBgamma(h) | AKT3 | Homo sapiens | 2.1 |
| PKCalpha(h) | PRKCA | Homo sapiens | 2.2 |
| PKCbetaI(h) | PRKCB | Homo sapiens | 1.0 |
| PKCbetaII(h) | PRKCB | Homo sapiens | 4.9 |
| PKCdelta(h) | PRKCD | Homo sapiens | -4.6 |
| PKCepsilon(h) | PRKCE | Homo sapiens | 11.0 |
| PKCeta(h) | PRKCH | Homo sapiens | 10.8 |
| PKCgamma(h) | PRKCG | Homo sapiens | -1.3 |
| PKCiota(h) | PRKCI | Homo sapiens | 0.2 |
| PKCmu(h) | PRKD1 | Homo sapiens | 5.3 |
| PKCtheta(h) | PRKCQ | Homo sapiens | 14.5 |
| PKCzeta(h) | PRKCZ | Homo sapiens | 8.3 |
| PKD2(h) | PRKD2 | Homo sapiens | 1.7 |
| PKD3(h) | PRKD3 | Homo sapiens | 1.7 |
| PKG1alpha(h) | PRKG1 | Homo sapiens | -0.2 |
| PKG1beta(h) | PRKG1 | Homo sapiens | -1.1 |
| PKR(h) | EIF2AK2 | Homo sapiens | -3.0 |
| Plk1(h) | PLK1 | Homo sapiens | -0.5 |
| Plk3(h) | PLK3 | Homo sapiens | -0.3 |
| Plk4(h) | PLK4 | Homo sapiens | 10.6 |
| PRAK(h) | MAPKAPK5 | Homo sapiens | 9.8 |
| PRK1(h) | PKN1 | Homo sapiens | -8.3 |
| PRK2(h) | PKN2 | Homo sapiens | 27.4 |
| PRKG2(h) | PRKG2 | Homo sapiens | -3.3 |
| PrKX(h) | PRKX | Homo sapiens | 6.2 |
| PRP4(h) | PRPF4B | Homo sapiens | -1.8 |
| PTK5(h) | FRK | Homo sapiens | 0.3 |
| Pyk2(h) | PTK2B | Homo sapiens | 3.6 |
| Ret(h) | RET | Homo sapiens | -9.4 |
| RIPK1(h) | RIPK1 | Homo sapiens | 2.0 |
| RIPK2(h) | RIPK2 | Homo sapiens | -2.3 |
| ROCK-I(h) | ROCK1 | Homo sapiens | -3.2 |
| ROCK-II(h) | ROCK2 | Homo sapiens | -11.4 |
| Ron(h) | MST1R | Homo sapiens | -7.9 |
| Ros(h) | ROS1 | Homo sapiens | 3.2 |
| Rse(h) | TYRO3 | Homo sapiens | -10.9 |
| Rsk1(h) | RPS6KA1 | Homo sapiens | -29.0 |
| Rsk2(h) | RPS6KA3 | Homo sapiens | -22.2 |
| Rsk3(h) | RPS6KA2 | Homo sapiens | -0.9 |
| Rsk4(h) | RPS6KA6 | Homo sapiens | -16.1 |
| SAPK2a(h) | MAPK14 | Homo sapiens | -19.0 |
| SAPK2b(h) | MAPK11 | Homo sapiens | -0.7 |
| SAPK3(h) | MAPK12 | Homo sapiens | -4.0 |
| SAPK4(h) | MAPK13 | Homo sapiens | -3.8 |
| SBK1(h) | SBK1 | Homo sapiens | 1.0 |
| SGK(h) | SGK1 | Homo sapiens | -12.3 |
| SGK2(h) | SGK2 | Homo sapiens | -3.4 |
| SGK3(h) | SGK3 | Homo sapiens | -5.1 |
| SIK(h) | SIK1 | Homo sapiens | -28.3 |
| SIK2(h) | SIK2 | Homo sapiens | 1.8 |
| SIK3(h) | SIK3 | Homo sapiens | -13.3 |
| SLK(h) | SLK | Homo sapiens | 0.2 |
| Snk(h) | PLK2 | Homo sapiens | 0.9 |
| SNRK(h) | SNRK | Homo sapiens | -13.4 |
| SRMS(h) | SRMS | Homo sapiens | 4.8 |
| SRPK1(h) | SRPK1 | Homo sapiens | -4.6 |
| SRPK2(h) | SRPK2 | Homo sapiens | -13.9 |
| STK16(h) | STK16 | Homo sapiens | -0.1 |
| STK25(h) | STK25 | Homo sapiens | 6.4 |
| STK32A(h) | STK32A | Homo sapiens | -1.1 |
| STK32B(h) | STK32B | Homo sapiens | -7.2 |
| STK32C(h) | STK32C | Homo sapiens | -3.0 |
| STK33(h) | STK33 | Homo sapiens | 6.2 |
| STK39(h) | STK39 | Homo sapiens | -4.7 |
| Syk(h) | SYK | Homo sapiens | -25.8 |
| TAF1L(h) | TAF1L | Homo sapiens | -2.4 |
| TAK1(h) | MAP3K7 | Homo sapiens | -1.6 |
| TAO1(h) | TAOK1 | Homo sapiens | 0.3 |
| TAO2(h) | TAOK2 | Homo sapiens | -6.4 |
| TAO3(h) | TAOK3 | Homo sapiens | 3.1 |
| TBK1(h) | TBK1 | Homo sapiens | 7.2 |
| Tec(h) activated | TEC | Homo sapiens | 2.9 |
| TGFBR1(h) | TGFBR1 | Homo sapiens | 3.4 |
| TGFBR2(h) | TGFBR2 | Homo sapiens | 8.3 |
| Tie2(h) | TEK | Homo sapiens | -14.5 |
| TLK1(h) | TLK1 | Homo sapiens | -21.8 |
| TLK2(h) | TLK2 | Homo sapiens | -6.6 |
| TNIK(h) | TNIK | Homo sapiens | -7.6 |
| TRB2(h) | TRIB2 | Homo sapiens | 3.5 |
| TrkA(h) | NTRK1 | Homo sapiens | -32.2 |
| TrkB(h) | NTRK2 | Homo sapiens | -25.5 |
| TrkC(h) | NTRK3 | Homo sapiens | 0.1 |
| TSSK1(h) | TSSK1B | Homo sapiens | 7.2 |
| TSSK2(h) | TSSK2 | Homo sapiens | 2.9 |
| TSSK3(h) | TSSK3 | Homo sapiens | -6.1 |
| TSSK4(h) | TSSK4 | Homo sapiens | -13.0 |
| TTBK1(h) | TTBK1 | Homo sapiens | -6.9 |
| TTBK2(h) | TTBK2 | Homo sapiens | -2.1 |
| TTK(h) | TTK | Homo sapiens | -7.1 |
| Txk(h) | TXK | Homo sapiens | -5.1 |
| TYK2(h) | TYK2 | Homo sapiens | 5.8 |
| ULK1(h) | ULK1 | Homo sapiens | -28.4 |
| ULK2(h) | ULK2 | Homo sapiens | 1.8 |
| ULK3(h) | ULK3 | Homo sapiens | 6.3 |
| VRK1(h) | VRK1 | Homo sapiens | 15.7 |
| VRK2(h) | VRK2 | Homo sapiens | 10.4 |
| WEE1(h) | WEE1 | Homo sapiens | -5.4 |
| Wee1B(h) | WEE2 | Homo sapiens | 7.6 |
| WNK1(h) | WNK1 | Homo sapiens | -5.4 |
| WNK2(h) | WNK2 | Homo sapiens | -13.2 |
| WNK3(h) | WNK3 | Homo sapiens | -2.6 |
| WNK4(h) | WNK4 | Homo sapiens | 2.5 |
| Yes(h) | YES1 | Homo sapiens | -2.7 |
| ZAK(h) | MAP3K20 | Homo sapiens | -13.7 |
| ZAP-70(h) | ZAP70 | Homo sapiens | 9.0 |
| ZIPK(h) | DAPK3 | Homo sapiens | 1.5 |
| ATM(h) | ATM | Homo sapiens | -1.9 |
| ATR/ATRIP(h) | ATR,ATRIP | Homo sapiens | 10.2 |
| DNA-PK(h) | PRKDC | Homo sapiens | -5.3 |
| PI3 Kinase (p110a/p85a)(h) | PIK3CA,PIK3R1 | Homo sapiens | -1.3 |
| PI3 Kinase (p110b/p85a)(h) | PIK3CB,PIK3R1 | Homo sapiens | -2.4 |
| PI3 Kinase (p110d/p85a)(h) | PIK3CD,PIK3R1 | Homo sapiens | -4.7 |
| PI3 Kinase (p120g)(h) | PIK3CG | Homo sapiens | 9.4 |
| PI3KC2a(h) | PIK3C2A | Homo sapiens | 27.5 |
| PI3KC2g(h) | PIK3C2G | Homo sapiens | 6.6 |
| PIP4K2a(h) | PIP4K2A | Homo sapiens | -2.8 |
| PIP5K1a(h) | PIP5K1A | Homo sapiens | -4.6 |
| PIP5K1g(h) | PIP5K1C | Homo sapiens | -0.4 |