Selectivity data for probe BAY 1816032 and control BAY-283
Jump to control PDSP data
BAY 1816032
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT1A | HTR1A | -21.37 | 9438.44 | 5.03 |
| 5-HT1E | HTR1E | -10.29 | ||
| 5-HT2A | HTR2A | -17.70 | ||
| 5-HT2B | HTR2B | 1.96 | ||
| 5-HT2C | HTR2C | -24.92 | ||
| 5-HT3 | HTR3A | -8.58 | ||
| 5-HT5A | HTR5A | -6.97 | ||
| 5-HT6 | HTR6 | -20.50 | ||
| 5-HT7A | HTR7 | -36.71 | > 10000.00 | < 5.00 |
| Alpha1A | ADRA1A | -38.23 | ||
| Alpha1B | ADRA1B | -19.65 | ||
| Alpha1D | ADRA1D | -53.48 | > 10000.00 | < 5.00 |
| Alpha2A | ADRA2A | 7.49 | ||
| Alpha2B | ADRA2B | -12.69 | ||
| Alpha2C | ADRA2C | -26.65 | > 10000.00 | < 5.00 |
| Beta1 | ADRB1 | -6.28 | ||
| Beta2 | ADRB2 | -15.32 | ||
| GABAA/BZP | 24.86 | |||
| D1 | DRD1 | -18.23 | ||
| D2 | DRD2 | 3.66 | ||
| D3 | DRD3 | 1.89 | ||
| D4 | DRD4 | 1.38 | ||
| D5 | DRD5 | -0.37 | ||
| DAT | SLC6A3 | 60.25 | > 10000.00 | < 5.00 |
| DOR | OPRD1 | -10.47 | ||
| H1 | HRH1 | 16.87 | ||
| H3 | HRH3 | 21.29 | ||
| H4 | HRH4 | 39.32 | ||
| KOR | OPRK1 | 15.23 | ||
| M1 | CHRM1 | -32.24 | ||
| M2 | CHRM2 | -17.08 | ||
| M3 | CHRM3 | -22.73 | ||
| M4 | CHRM4 | -34.40 | ||
| M5 | CHRM5 | 8.89 | ||
| MOR | OPRM1 | -4.25 | ||
| NET | SLC6A2 | -11.03 | ||
| GABA/PBR | -24.28 | |||
| SERT | SLC6A4 | -28.91 | ||
| Sigma 1 | SIGMAR1 | 4.34 | ||
| Sigma 2 | TMEM97 | 13.00 | ||
| 5-HT1B | HTR1B | 11.79 | ||
| 5-HT1D | HTR1D | 9.30 | ||
| Beta3 | ADRB3 | 4.26 | ||
| H2 | HRH2 | 9.79 |
BAY-283
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT1A | HTR1A | 12.26 | ||
| 5-HT1E | HTR1E | -3.71 | ||
| 5-HT2A | HTR2A | 6.50 | ||
| 5-HT2B | HTR2B | -3.83 | ||
| 5-HT2C | HTR2C | -11.29 | ||
| 5-HT3 | HTR3A | -3.97 | ||
| 5-HT5A | HTR5A | 3.77 | ||
| 5-HT6 | HTR6 | -43.44 | > 10000.00 | < 5.00 |
| 5-HT7A | HTR7 | -3.39 | ||
| Alpha1A | ADRA1A | -6.10 | ||
| Alpha1B | ADRA1B | -4.46 | ||
| Alpha1D | ADRA1D | 12.86 | ||
| Alpha2A | ADRA2A | 28.90 | ||
| Alpha2B | ADRA2B | 27.64 | ||
| Alpha2C | ADRA2C | 12.91 | ||
| Beta1 | ADRB1 | 1.17 | ||
| Beta2 | ADRB2 | -13.43 | ||
| GABAA/BZP | -19.68 | |||
| D1 | DRD1 | 41.33 | ||
| D2 | DRD2 | 21.79 | ||
| D3 | DRD3 | 20.03 | ||
| D4 | DRD4 | 24.85 | ||
| D5 | DRD5 | 26.84 | ||
| DAT | SLC6A3 | 82.80 | 1626.67 | 5.79 |
| DOR | OPRD1 | -9.55 | ||
| H1 | HRH1 | 20.28 | ||
| H3 | HRH3 | -10.68 | ||
| H4 | HRH4 | 27.77 | ||
| KOR | OPRK1 | 17.50 | ||
| M1 | CHRM1 | -14.29 | ||
| M2 | CHRM2 | -12.11 | ||
| M3 | CHRM3 | -23.78 | ||
| M4 | CHRM4 | 9.26 | ||
| M5 | CHRM5 | -14.30 | ||
| MOR | OPRM1 | -9.70 | ||
| NET | SLC6A2 | 58.69 | 2744.73 | 5.56 |
| GABA/PBR | 13.87 | |||
| SERT | SLC6A4 | 10.90 | ||
| Sigma 1 | SIGMAR1 | 52.24 | 1340.29 | 5.87 |
| Sigma 2 | TMEM97 | 69.23 | 655.24 | 6.18 |
| 5-HT1B | HTR1B | 33.79 | ||
| 5-HT1D | HTR1D | 55.07 | 8973.80 average (n=2) | 5.05 |
| Beta3 | ADRB3 | 33.64 | ||
| H2 | HRH2 | 28.69 |
BAY 1816032
Results are significant for > 50 % inhibition.
Conclusion: Closest off-targets [% inh.] are human Adenosine transporter (71, IC50 = 370 nM; 51-fold), ADORA2A (67) and GABAA Chloride Channel TBOB receptor (60).
| Target protein | HGNC name | Species | Cmp. conc. | % inhibition | Reference compound name | Reference compound IC50 [nM] | Assay ID |
|---|---|---|---|---|---|---|---|
| GABAA, Chloride Channel, TBOB | Rattus sp. | 10 µM | 60.0 | Picrotoxin | 270.00 | 226810 | |
| Adenosine A2A | ADORA2A | Homo sapiens | 10 µM | 67.0 | CGS-21680 | 130.00 | 200610 |
| Transporter, Adenosine | Cavia porcellus | 10 µM | 71.0 | Nitrobenzylthioinosine | 0.85 | 202000 | |
| Sodium Channel, Site 2 | Rattus sp. | 10 µM | 53.0 | Dibucaine | 61.00 | 279510 | |
| Adenosine A1 | ADORA1 | Homo sapiens | 10 µM | 9.0 | R(-)-PIA | 830.00 | 200510 |
| Adrenergic alpha1A | ADRA1A | Rattus sp. | 10 µM | 8.0 | Prazosin | 0.69 | 203100 |
| Adrenergic alpha1B | ADRA1B | Rattus sp. | 10 µM | -6.0 | Prazosin | 0.27 | 203200 |
| Adrenergic alpha1D | ADRA1D | Homo sapiens | 10 µM | 24.0 | Prazosin | 0.88 | 203400 |
| Adrenergic alpha2A | ADRA2A | Homo sapiens | 10 µM | 2.0 | Yohimbine | 1.80 | 203630 |
| Adrenergic alpha2B | ADRA2B | Homo sapiens | 10 µM | -15.0 | Yohimbine | 14.00 | 203710 |
| Adrenergic beta1 | ADRB1 | Homo sapiens | 10 µM | 4.0 | S(-)-Propranolol | 2.50 | 204010 |
| Adrenergic beta2 | ADRB2 | Homo sapiens | 10 µM | 10.0 | S(-)-Propranolol | 0.78 | 204110 |
| Androgen (Testosterone) AR | AR | Homo sapiens | 10 µM | 9.0 | Testosterone | 2.10 | 206000 |
| Angiotensin AT1 | AGTR1 | Homo sapiens | 10 µM | -2.0 | 299020 | ||
| Bradykinin B2 | BDKRB2 | Homo sapiens | 10 µM | 0.0 | 299021 | ||
| Calcium Channel L-Type, Benzothiazepine | CACNA1C | Rattus sp. | 10 µM | -10.0 | Diltiazem | 0.04 | 214510 |
| Calcium Channel L-Type, Dihydropyridine | CACNA1C | Rattus sp. | 10 µM | 8.0 | Nitrendipine | 0.72 | 214600 |
| Calcium Channel L-Type, Phenylalkylamine | CACNA1C | Rattus sp. | 10 µM | 14.0 | 299019 | ||
| Calcium Channel N-Type | CACNA1B | Rattus sp. | 10 µM | 10.0 | omega-Conotoxin GVIA | 0.03 | 216000 |
| Cannabinoid CB1 | CNR1 | Homo sapiens | 10 µM | -6.0 | R(+)-WIN-55,212-2 | 200.00 | 217030 |
| Cannabinoid CB2 | CNR2 | Homo sapiens | 10 µM | 31.0 | R(+)-WIN-55,212-2 | 5.80 | 217100 |
| Chemokine CCR1 | CCR1 | Homo sapiens | 10 µM | -4.0 | MCP-3 | 0.27 | 217510 |
| Chemokine CXCR2 (IL-8RB) | CXCR2 | Homo sapiens | 10 µM | -3.0 | 299023 | ||
| Cholecystokinin CCK1 (CCKA) | CCKAR | Homo sapiens | 10 µM | -19.0 | Lintitript (SR 27897) | 0.93 | 218030 |
| Cholecystokinin CCK2 (CCKB) | CCKBR | Homo sapiens | 10 µM | 1.0 | 216130 | ||
| Dopamine D1 | DRD1 | Homo sapiens | 10 µM | 5.0 | R(+)-SCH-23390 | 1.40 | 219500 |
| Dopamine D2L | DRD2 | Homo sapiens | 10 µM | 4.0 | Spiperone | 0.26 | 219600 |
| Dopamine D2S | DRD2 | Homo sapiens | 10 µM | 17.0 | Spiperone | 0.25 | 219700 |
| Endothelin ETA | EDNRA | Homo sapiens | 10 µM | -23.0 | 299027 | ||
| Estrogen ERalpha | ESR1 | Homo sapiens | 10 µM | 10.0 | Diethylstilbestrol | 0.77 | 226010 |
| GABAA, Flunitrazepam, Central | Rattus sp. | 10 µM | 7.0 | Hydrogen diazepam chloride | 16.00 | 226600 | |
| GABAA, Ro-15-1788, Hippocampus | Rattus sp. | 10 µM | 22.0 | Diazepam | 46.00 | 226630 | |
| GABAB1A | GABBR1 | Homo sapiens | 10 µM | -2.0 | Cgp-54626 | 6.40 | 228610 |
| Glucocorticoid | NR3C1 | Homo sapiens | 10 µM | -24.0 | Dexamethasone | 3.80 | 232030 |
| Glutamate, AMPA | Rattus sp. | 10 µM | 7.0 | L-Glutamic acid | 320.00 | 232600 | |
| Glutamate, Kainate | GRIK2 | Rattus sp. | 10 µM | -1.0 | L-Glutamic acid | 240.00 | 232700 |
| Glutamate, Metabotropic, mGlu5 | GRM5 | Homo sapiens | 10 µM | 17.0 | L-Glutamic acid | 1500.00 | 237000 |
| Glutamate, NMDA, Agonism | Rattus sp. | 10 µM | 4.0 | L-Glutamic acid | 410.00 | 232810 | |
| Glutamate, NMDA, Glycine | Rattus sp. | 10 µM | -2.0 | MDL 105,519 | 22.00 | 232910 | |
| Glutamate, NMDA, Phencyclidine | Rattus sp. | 10 µM | 2.0 | Dizolcipine ((+)-MK- 801) | 5.10 | 233000 | |
| Glutamate, NMDA, Polyamine | Rattus sp. | 10 µM | 0.0 | Ifenprodil | 23.00 | 234000 | |
| Glycine, Strychnine-Sensitive | Rattus sp. | 10 µM | 0.0 | (-)-Strychnine | 8.90 | 239000 | |
| Histamine H1 | HRH1 | Homo sapiens | 10 µM | 12.0 | Pyrilamine | 3.30 | 239610 |
| Histamine H2 | HRH2 | Homo sapiens | 10 µM | -13.0 | 299012 | ||
| Leukotriene, Cysteinyl CysLT1 | CYSLTR1 | Homo sapiens | 10 µM | 32.0 | Leukotriene D4 | 0.70 | 250460 |
| Melanocortin MC1 | MC1R | Homo sapiens | 10 µM | 4.0 | NDP-alpha-MSH | 0.06 | 251100 |
| Melanocortin MC4 | MC4R | Homo sapiens | 10 µM | 10.0 | 299024 | ||
| Muscarinic M1 | CHRM1 | Homo sapiens | 10 µM | 32.0 | 299029 | ||
| Muscarinic M2 | CHRM2 | Homo sapiens | 10 µM | -20.0 | 4-DAMP | 55.00 | 252710 |
| Muscarinic M3 | CHRM3 | Homo sapiens | 10 µM | -5.0 | 4-DAMP | 5.10 | 252810 |
| Muscarinic M4 | CHRM4 | Homo sapiens | 10 µM | 8.0 | 4-DAMP | 15.00 | 252910 |
| Neuropeptide Y Y1 | NPY1R | Homo sapiens | 10 µM | -11.0 | 299011 | ||
| Nicotinic Acetylcholine | Homo sapiens | 10 µM | -15.0 | Epibatidine | 0.08 | 258590 | |
| Nicotinic Acetylcholine D1, Bungarotoxin | CHRNA1 | Homo sapiens | 10 µM | 14.0 | alpha-Bungarotoxin | 1.10 | 258700 |
| Opiate delta1 (OP1, DOP) | OPRD1 | Homo sapiens | 10 µM | -6.0 | Naltrindole | 0.91 | 260130 |
| Opiate kappa (OP2, KOP) | OPRK1 | Homo sapiens | 10 µM | 26.0 | U-69593 | 16.00 | 260210 |
| Opiate µ (OP3, MOP) | OPRM1 | Homo sapiens | 10 µM | -37.0 | DAMGO | 20.00 | 260410 |
| Platelet Activating Factor (PAF) | PTAFR | Homo sapiens | 10 µM | 28.0 | PAF | 0.28 | 265010 |
| Potassium Channel [KATP] | KCNJ11 | Cricetinae | 10 µM | 4.0 | Glyburide | 5.70 | 265600 |
| Potassium Channel hERG | KCNH2 | Homo sapiens | 10 µM | 23.0 | Astemizole | 265900 | |
| PPARgamma | PPARG | Homo sapiens | 10 µM | -8.0 | Rosiglitazone | 39.00 | 267500 |
| Progesterone PR-B | PGR | Homo sapiens | 10 µM | -12.0 | R-5020 | 0.49 | 299005 |
| Serotonin (5-Hydroxytryptamine) 5-HT1A | HTR1A | Homo sapiens | 10 µM | 0.0 | 299013 | ||
| Serotonin (5-Hydroxytryptamine) 5-HT1B | HTR1B | Homo sapiens | 10 µM | 15.0 | Serotonin (5-HT) | 150.00 | 271230 |
| Serotonin (5-Hydroxytryptamine) 5-HT2A | HTR2A | Homo sapiens | 10 µM | 22.0 | 299014 | ||
| Serotonin (5-Hydroxytryptamine) 5-HT2B | HTR2B | Homo sapiens | 10 µM | 22.0 | Ketanserin | 290.00 | 271700 |
| Serotonin (5-Hydroxytryptamine) 5-HT2C | HTR2C | Homo sapiens | 10 µM | 21.0 | SBZ4Z084 | 1.00 | 271800 |
| Serotonin (5-Hydroxytryptamine) 5-HT3 | HTR3A | Homo sapiens | 10 µM | -3.0 | MDL-72222 | 11.00 | 299022 |
| Tachykinin NK1 | TACR1 | Homo sapiens | 10 µM | 19.0 | L-703606 | 3.60 | 255520 |
| Transporter, Dopamine (DAT) | SLC6A3 | Homo sapiens | 10 µM | -5.0 | GBR-12909 | 1.70 | 299026 |
| Transporter, GABA | Rattus sp. | 10 µM | 1.0 | NO-711 | 200.00 | 226400 | |
| Transporter, Norepinephrine (NET) | SLC6A2 | Homo sapiens | 10 µM | 26.0 | Desipramine | 0.93 | 204410 |
| Transporter, Serotonin (5- Hydroxytryptamine) (SERT) | SLC6A4 | Homo sapiens | 10 µM | 4.0 | 299025 | ||
| Vasopressin V1A | AVPR1A | Homo sapiens | 10 µM | 11.0 | 299018 |
BAY 1816032
Results are significant for > 50 % inhibition.
Conclusion: Clean panel.
| Target protein | HGNC name | Species | Cmp. conc. | % inhibition | Reference compound name | Reference compound IC50 [µM] | Assay ID |
|---|---|---|---|---|---|---|---|
| Cyclooxygenase COX-1 | PTGS1 | Homo sapiens | 10 µM | 54.0 | Indomethacin | 0.04 | 116020 |
| Phosphodiesterase PDE4 | Homo sapiens | 10 µM | 52.0 | Ro 20-1724 | 1.10 | 154000 | |
| ATPase, Na+/K+, Heart | Sus scrofa | 10 µM | 21.0 | Ouabain | 2.00 | 107710 | |
| Cholinesterase, Acetyl, ACES | ACHE | Homo sapiens | 10 µM | 2.0 | Physostigmine | 0.12 | 104010 |
| Cyclooxygenase COX-2 | PTGS2 | Homo sapiens | 10 µM | -9.0 | Rofecoxib | 0.42 | 118030 |
| Monoamine Oxidase MAO-A | MAOA | Homo sapiens | 10 µM | 7.0 | Clorgyline | 0.00 | 140010 |
| Monoamine Oxidase MAO-B | MAOB | Homo sapiens | 10 µM | -15.0 | R(-)-Deprenyl | 0.01 | 140120 |
| Peptidase, Angiotensin Converting Enzyme | ACE | Oryctolagus cuniculus | 10 µM | -4.0 | Captopril | 0.01 | 107300 |
| Peptidase, CTSG (Cathepsin G) | CTSG | Homo sapiens | 10 µM | -15.0 | Chymostatin | 2.10 | 112510 |
| Phosphodiesterase PDE3 | Homo sapiens | 10 µM | 4.0 | Cilostamide | 0.05 | 152000 | |
| Protein Serine/Threonine Kinase, PKC, Non-Selective | Rattus sp. | 10 µM | -12.0 | Staurosporine | 0.00 | 178010 | |
| Protein Tyrosine Kinase, Insulin Receptor | INSR | Homo sapiens | 10 µM | -12.0 | GSK 1838705 | 0.01 | 174990 |
| Protein Tyrosine Kinase, LCK | LCK | Homo sapiens | 10 µM | 6.0 | TC-S 7003 | 0.06 | 176020 |
BAY 1816032
Data is expressed as % of control: 100% = no competition with immobilized ligand, 0% full competition with immobilized ligand. Shown are data from PMID: 30429199 (Supplementary Table 1) .
Conclusion: Closest off-targets are STK10 (Kd = 57 nM; 17-fold), CDC42BPG CDC42BPG (Kd = 850 nM; > 250 fold).
| Target protein | HGNC name | Species | % inhibition at 1 µM | Kd [nM] |
|---|---|---|---|---|
| CDKL1 | CDKL1 | Homo sapiens | 81.0 | |
| MAP4K5 | MAP4K5 | Homo sapiens | 81.0 | |
| BUB1 | BUB1 | Homo sapiens | 0.1 | 3.30 |
| LOK | STK10 | Homo sapiens | 0.6 | 57.00 |
| DYRK1B | DYRK1B | Homo sapiens | 6.7 | > 30000.00 |
| DDR1 | DDR1 | Homo sapiens | 21.0 | 2300.00 |
| DMPK2 | CDC42BPG | Homo sapiens | 22.0 | 850.00 |
| GSK3A | GSK3A | Homo sapiens | 26.0 | > 30000.00 |
| JNK2 | MAPK9 | Homo sapiens | 39.0 | |
| TIE2 | TEK | Homo sapiens | 41.0 | |
| ZAK | MAP3K20 | Homo sapiens | 42.0 | |
| AXL | AXL | Homo sapiens | 47.0 | |
| CSNK2A2 | CSNK2A2 | Homo sapiens | 48.0 | |
| CAMK1 | CAMK1 | Homo sapiens | 52.0 | |
| CIT | CIT | Homo sapiens | 52.0 | |
| LZK | MAP3K13 | Homo sapiens | 53.0 | |
| TGFBR1 | TGFBR1 | Homo sapiens | 53.0 | |
| VPS34 | PIK3C3 | Homo sapiens | 55.0 | |
| JNK3 | MAPK10 | Homo sapiens | 56.0 | |
| TYRO3 | TYRO3 | Homo sapiens | 56.0 | |
| TESK1 | TESK1 | Homo sapiens | 57.0 | |
| CAMK2A | CAMK2A | Homo sapiens | 58.0 | |
| GRK7 | GRK7 | Homo sapiens | 60.0 | |
| MAP4K4 | MAP4K4 | Homo sapiens | 62.0 | |
| TNK1 | TNK1 | Homo sapiens | 62.0 | |
| TTK | TTK | Homo sapiens | 62.0 | |
| MAST1 | MAST1 | Homo sapiens | 63.0 | |
| WNK4 | WNK4 | Homo sapiens | 63.0 | |
| TXK | TXK | Homo sapiens | 64.0 | |
| EPHA1 | EPHA1 | Homo sapiens | 65.0 | |
| STK16 | STK16 | Homo sapiens | 65.0 | |
| TIE1 | TIE1 | Homo sapiens | 65.0 | |
| MARK2 | MARK2 | Homo sapiens | 67.0 | |
| CAMK4 | CAMK4 | Homo sapiens | 68.0 | |
| CSNK1D | CSNK1D | Homo sapiens | 68.0 | |
| STK36 | STK36 | Homo sapiens | 68.0 | |
| ACVRL1 | ACVRL1 | Homo sapiens | 69.0 | |
| CDK8 | CDK8 | Homo sapiens | 69.0 | |
| MYLK2 | MYLK2 | Homo sapiens | 69.0 | |
| ERBB3 | ERBB3 | Homo sapiens | 70.0 | |
| NEK6 | NEK6 | Homo sapiens | 70.0 | |
| RIPK4 | RIPK4 | Homo sapiens | 70.0 | |
| MEK5 | MAP2K5 | Homo sapiens | 71.0 | |
| RAF1 | RAF1 | Homo sapiens | 71.0 | |
| YANK1 | STK32A | Homo sapiens | 71.0 | |
| ACVR1B | ACVR1B | Homo sapiens | 72.0 | |
| MLCK | MYLK3 | Homo sapiens | 72.0 | |
| MRCKA | CDC42BPA | Homo sapiens | 72.0 | |
| YANK3 | STK32C | Homo sapiens | 72.0 | |
| MAK | MAK | Homo sapiens | 73.0 | |
| MARK3 | MARK3 | Homo sapiens | 73.0 | |
| BIKE | BMP2K | Homo sapiens | 74.0 | |
| BMPR1A | BMPR1A | Homo sapiens | 74.0 | |
| CSNK1G1 | CSNK1G1 | Homo sapiens | 74.0 | |
| PRKG1 | PRKG1 | Homo sapiens | 74.0 | |
| MINK | MINK1 | Homo sapiens | 76.0 | |
| MLK2 | MAP3K10 | Homo sapiens | 76.0 | |
| PCTK3 | CDK18 | Homo sapiens | 76.0 | |
| YSK1 | STK25 | Homo sapiens | 76.0 | |
| CSK | CSK | Homo sapiens | 77.0 | |
| GAK | GAK | Homo sapiens | 77.0 | |
| HPK1 | MAP4K1 | Homo sapiens | 77.0 | |
| PDGFRB | PDGFRB | Homo sapiens | 77.0 | |
| PRKCQ | PRKCQ | Homo sapiens | 77.0 | |
| SRPK2 | SRPK2 | Homo sapiens | 77.0 | |
| CASK | CASK | Homo sapiens | 78.0 | |
| CDK11 | CDK19 | Homo sapiens | 78.0 | |
| CSNK1G2 | CSNK1G2 | Homo sapiens | 78.0 | |
| EPHA5 | EPHA5 | Homo sapiens | 78.0 | |
| NDR2 | STK38L | Homo sapiens | 78.0 | |
| NEK1 | NEK1 | Homo sapiens | 78.0 | |
| NEK7 | NEK7 | Homo sapiens | 78.0 | |
| GRK4 | GRK4 | Homo sapiens | 79.0 | |
| JNK1 | MAPK8 | Homo sapiens | 79.0 | |
| PAK6 | PAK6 | Homo sapiens | 79.0 | |
| PRKD3 | PRKD3 | Homo sapiens | 79.0 | |
| RIOK1 | RIOK1 | Homo sapiens | 79.0 | |
| FES | FES | Homo sapiens | 80.0 | |
| MAP3K4 | MAP3K4 | Homo sapiens | 80.0 | |
| MET | MET | Homo sapiens | 80.0 | |
| MST1R | MST1R | Homo sapiens | 80.0 | |
| PIK3CG | PIK3CG | Homo sapiens | 80.0 | |
| PRKCD | PRKCD | Homo sapiens | 80.0 | |
| RSK1(Kin.Dom.1-N-terminal) | RPS6KA1 | Homo sapiens | 80.0 | |
| RSK3(Kin.Dom.1-N-terminal) | RPS6KA2 | Homo sapiens | 80.0 | |
| CDK5 | CDK5 | Homo sapiens | 81.0 | |
| PAK3 | PAK3 | Homo sapiens | 81.0 | |
| ASK2 | MAP3K6 | Homo sapiens | 82.0 | |
| FLT4 | FLT4 | Homo sapiens | 82.0 | |
| KIT | KIT | Homo sapiens | 82.0 | |
| MST2 | STK3 | Homo sapiens | 82.0 | |
| NEK9 | NEK9 | Homo sapiens | 82.0 | |
| p38-beta | MAPK11 | Homo sapiens | 82.0 | |
| PAK4 | PAK4 | Homo sapiens | 82.0 | |
| RIPK2 | RIPK2 | Homo sapiens | 82.0 | |
| TRPM6 | TRPM6 | Homo sapiens | 82.0 | |
| YANK2 | STK32B | Homo sapiens | 82.0 | |
| BRSK2 | BRSK2 | Homo sapiens | 83.0 | |
| CAMK1D | CAMK1D | Homo sapiens | 83.0 | |
| CLK4 | CLK4 | Homo sapiens | 83.0 | |
| DRAK2 | STK17B | Homo sapiens | 83.0 | |
| MERTK | MERTK | Homo sapiens | 83.0 | |
| p38-gamma | MAPK12 | Homo sapiens | 83.0 | |
| PIP5K1A | PIP5K1A | Homo sapiens | 83.0 | |
| DAPK3 | DAPK3 | Homo sapiens | 84.0 | |
| ICK | CILK1 | Homo sapiens | 84.0 | |
| MELK | MELK | Homo sapiens | 84.0 | |
| SIK | SIK1 | Homo sapiens | 84.0 | |
| DAPK2 | DAPK2 | Homo sapiens | 85.0 | |
| EPHA3 | EPHA3 | Homo sapiens | 85.0 | |
| FRK | FRK | Homo sapiens | 85.0 | |
| PAK7 | PAK5 | Homo sapiens | 85.0 | |
| TLK1 | TLK1 | Homo sapiens | 85.0 | |
| WNK1 | WNK1 | Homo sapiens | 85.0 | |
| LIMK1 | LIMK1 | Homo sapiens | 86.0 | |
| ABL1-nonphosphorylated | ABL1 | Homo sapiens | 87.0 | |
| DLK | MAP3K12 | Homo sapiens | 87.0 | |
| EIF2AK1 | EIF2AK1 | Homo sapiens | 87.0 | |
| FGFR1 | FGFR1 | Homo sapiens | 87.0 | |
| JAK3(JH1domain-catalytic) | JAK3 | Homo sapiens | 87.0 | |
| MAP3K15 | MAP3K15 | Homo sapiens | 87.0 | |
| PCTK2 | CDK17 | Homo sapiens | 87.0 | |
| PFTK1 | CDK14 | Homo sapiens | 87.0 | |
| PIK4CB | PI4KB | Homo sapiens | 87.0 | |
| PRKCI | PRKCI | Homo sapiens | 87.0 | |
| SRPK3 | SRPK3 | Homo sapiens | 87.0 | |
| WNK3 | WNK3 | Homo sapiens | 87.0 | |
| AKT2 | AKT2 | Homo sapiens | 88.0 | |
| BLK | BLK | Homo sapiens | 88.0 | |
| ERK1 | MAPK3 | Homo sapiens | 88.0 | |
| FAK | PTK2 | Homo sapiens | 88.0 | |
| FLT3 | FLT3 | Homo sapiens | 88.0 | |
| NEK5 | NEK5 | Homo sapiens | 88.0 | |
| NIM1 | NIM1K | Homo sapiens | 88.0 | |
| NLK | NLK | Homo sapiens | 88.0 | |
| PIKFYVE | PIKFYVE | Homo sapiens | 88.0 | |
| PRKR | EIF2AK2 | Homo sapiens | 88.0 | |
| CDK2 | CDK2 | Homo sapiens | 89.0 | |
| CDKL3 | CDKL3 | Homo sapiens | 89.0 | |
| CSNK1A1L | CSNK1A1L | Homo sapiens | 89.0 | |
| EPHA6 | EPHA6 | Homo sapiens | 89.0 | |
| FLT1 | FLT1 | Homo sapiens | 89.0 | |
| FYN | FYN | Homo sapiens | 89.0 | |
| MEK6 | MAP2K6 | Homo sapiens | 89.0 | |
| PRKCH | PRKCH | Homo sapiens | 89.0 | |
| CDKL2 | CDKL2 | Homo sapiens | 90.0 | |
| DCAMKL2 | DCLK2 | Homo sapiens | 90.0 | |
| HIPK4 | HIPK4 | Homo sapiens | 90.0 | |
| JAK1(JH1domain-catalytic) | JAK1 | Homo sapiens | 90.0 | |
| MEK4 | MAP2K4 | Homo sapiens | 90.0 | |
| NEK2 | NEK2 | Homo sapiens | 90.0 | |
| RIOK3 | RIOK3 | Homo sapiens | 90.0 | |
| SRPK1 | SRPK1 | Homo sapiens | 90.0 | |
| TSSK3 | TSSK3 | Homo sapiens | 90.0 | |
| ULK1 | ULK1 | Homo sapiens | 90.0 | |
| BRK | PTK6 | Homo sapiens | 91.0 | |
| CDC2L1 | CDK11B | Homo sapiens | 91.0 | |
| GCN2(Kin.Dom.2,S808G) | EIF2AK4 | Homo sapiens | 91.0 | |
| MYO3B | MYO3B | Homo sapiens | 91.0 | |
| PIP5K2B | PIP4K2B | Homo sapiens | 91.0 | |
| RPS6KA4(Kin.Dom.1-N-terminal) | RPS6KA4 | Homo sapiens | 91.0 | |
| WNK2 | WNK2 | Homo sapiens | 91.0 | |
| ARK5 | NUAK1 | Homo sapiens | 92.0 | |
| FGR | FGR | Homo sapiens | 92.0 | |
| IKK-epsilon | IKBKE | Homo sapiens | 92.0 | |
| IRAK3 | IRAK3 | Homo sapiens | 92.0 | |
| MAP3K1 | MAP3K1 | Homo sapiens | 92.0 | |
| MAPKAPK2 | MAPKAPK2 | Homo sapiens | 92.0 | |
| MLK1 | MAP3K9 | Homo sapiens | 92.0 | |
| PKN1 | PKN1 | Homo sapiens | 92.0 | |
| TRKA | NTRK1 | Homo sapiens | 92.0 | |
| BRSK1 | BRSK1 | Homo sapiens | 93.0 | |
| CHEK1 | CHEK1 | Homo sapiens | 93.0 | |
| DDR2 | DDR2 | Homo sapiens | 93.0 | |
| EPHB4 | EPHB4 | Homo sapiens | 93.0 | |
| ERK2 | MAPK1 | Homo sapiens | 93.0 | |
| ERK3 | MAPK6 | Homo sapiens | 93.0 | |
| MUSK | MUSK | Homo sapiens | 93.0 | |
| SGK | SGK1 | Homo sapiens | 93.0 | |
| ABL1-phosphorylated | ABL1 | Homo sapiens | 94.0 | |
| ACVR2B | ACVR2B | Homo sapiens | 94.0 | |
| ERK5 | MAPK7 | Homo sapiens | 94.0 | |
| HIPK1 | HIPK1 | Homo sapiens | 94.0 | |
| MEK2 | MAP2K2 | Homo sapiens | 94.0 | |
| TBK1 | TBK1 | Homo sapiens | 94.0 | |
| VRK2 | VRK2 | Homo sapiens | 94.0 | |
| AMPK-alpha2 | PRKAA2 | Homo sapiens | 95.0 | |
| ASK1 | MAP3K5 | Homo sapiens | 95.0 | |
| CAMK1B | PNCK | Homo sapiens | 95.0 | |
| DRAK1 | STK17A | Homo sapiens | 95.0 | |
| EPHB3 | EPHB3 | Homo sapiens | 95.0 | |
| LATS1 | LATS1 | Homo sapiens | 95.0 | |
| MAP3K3 | MAP3K3 | Homo sapiens | 95.0 | |
| PRKG2 | PRKG2 | Homo sapiens | 95.0 | |
| PYK2 | PTK2B | Homo sapiens | 95.0 | |
| DYRK1A | DYRK1A | Homo sapiens | 96.0 | |
| EPHA4 | EPHA4 | Homo sapiens | 96.0 | |
| ERK4 | MAPK4 | Homo sapiens | 96.0 | |
| INSRR | INSRR | Homo sapiens | 96.0 | |
| NEK11 | NEK11 | Homo sapiens | 96.0 | |
| PFTAIRE2 | CDK15 | Homo sapiens | 96.0 | |
| PRP4 | PRPF4B | Homo sapiens | 96.0 | |
| SNRK | SNRK | Homo sapiens | 96.0 | |
| TLK2 | TLK2 | Homo sapiens | 96.0 | |
| CTK | MATK | Homo sapiens | 97.0 | |
| IGF1R | IGF1R | Homo sapiens | 97.0 | |
| INSR | INSR | Homo sapiens | 97.0 | |
| LIMK2 | LIMK2 | Homo sapiens | 97.0 | |
| MAP3K2 | MAP3K2 | Homo sapiens | 97.0 | |
| MARK1 | MARK1 | Homo sapiens | 97.0 | |
| MEK1 | MAP2K1 | Homo sapiens | 97.0 | |
| PIK3CB | PIK3CB | Homo sapiens | 97.0 | |
| PKN2 | PKN2 | Homo sapiens | 97.0 | |
| RET | RET | Homo sapiens | 97.0 | |
| RIPK1 | RIPK1 | Homo sapiens | 97.0 | |
| STK39 | STK39 | Homo sapiens | 97.0 | |
| TNNI3K | TNNI3K | Homo sapiens | 97.0 | |
| WEE2 | WEE2 | Homo sapiens | 97.0 | |
| YSK4 | MAP3K19 | Homo sapiens | 97.0 | |
| ACVR1 | ACVR1 | Homo sapiens | 98.0 | |
| ADCK3 | COQ8A | Homo sapiens | 98.0 | |
| EPHA7 | EPHA7 | Homo sapiens | 98.0 | |
| FGFR4 | FGFR4 | Homo sapiens | 98.0 | |
| MKK7 | MAP2K7 | Homo sapiens | 98.0 | |
| MRCKB | CDC42BPB | Homo sapiens | 98.0 | |
| NDR1 | STK38 | Homo sapiens | 98.0 | |
| PHKG2 | PHKG2 | Homo sapiens | 98.0 | |
| PIK3C2G | PIK3C2G | Homo sapiens | 98.0 | |
| PLK1 | PLK1 | Homo sapiens | 98.0 | |
| RSK2(Kin.Dom.2-C-terminal) | RPS6KA3 | Homo sapiens | 98.0 | |
| TRKC | NTRK3 | Homo sapiens | 98.0 | |
| ADCK4 | COQ8B | Homo sapiens | 99.0 | |
| BRAF | BRAF | Homo sapiens | 99.0 | |
| CAMK1G | CAMK1G | Homo sapiens | 99.0 | |
| CDK3 | CDK3 | Homo sapiens | 99.0 | |
| CDK9 | CDK9 | Homo sapiens | 99.0 | |
| CSF1R | CSF1R | Homo sapiens | 99.0 | |
| CSNK1A1 | CSNK1A1 | Homo sapiens | 99.0 | |
| HUNK | HUNK | Homo sapiens | 99.0 | |
| NEK4 | NEK4 | Homo sapiens | 99.0 | |
| p38-delta | MAPK13 | Homo sapiens | 99.0 | |
| SGK3 | SGK3 | Homo sapiens | 99.0 | |
| SNARK | NUAK2 | Homo sapiens | 99.0 | |
| STK35 | STK35 | Homo sapiens | 99.0 | |
| AAK1 | AAK1 | Homo sapiens | 100.0 | |
| ABL2 | ABL2 | Homo sapiens | 100.0 | |
| ACVR2A | ACVR2A | Homo sapiens | 100.0 | |
| AKT1 | AKT1 | Homo sapiens | 100.0 | |
| AKT3 | AKT3 | Homo sapiens | 100.0 | |
| ALK | ALK | Homo sapiens | 100.0 | |
| AMPK-alpha1 | PRKAA1 | Homo sapiens | 100.0 | |
| ANKK1 | ANKK1 | Homo sapiens | 100.0 | |
| AURKA | AURKA | Homo sapiens | 100.0 | |
| AURKB | AURKB | Homo sapiens | 100.0 | |
| AURKC | AURKC | Homo sapiens | 100.0 | |
| BMPR1B | BMPR1B | Homo sapiens | 100.0 | |
| BMPR2 | BMPR2 | Homo sapiens | 100.0 | |
| BMX | BMX | Homo sapiens | 100.0 | |
| BTK | BTK | Homo sapiens | 100.0 | |
| CAMK2B | CAMK2B | Homo sapiens | 100.0 | |
| CAMK2D | CAMK2D | Homo sapiens | 100.0 | |
| CAMK2G | CAMK2G | Homo sapiens | 100.0 | |
| CAMKK1 | CAMKK1 | Homo sapiens | 100.0 | |
| CAMKK2 | CAMKK2 | Homo sapiens | 100.0 | |
| CDC2L2 | CDK11A | Homo sapiens | 100.0 | |
| CDC2L5 | CDK13 | Homo sapiens | 100.0 | |
| CDK4 | CDK4 | Homo sapiens | 100.0 | |
| CDK4-cyclinD1 |
CDK4 CCND1 |
Homo sapiens | 100.0 | |
| CDK4-cyclinD3 |
CDK4 CCND3 |
Homo sapiens | 100.0 | |
| CDK7 | CDK7 | Homo sapiens | 100.0 | |
| CDKL5 | CDKL5 | Homo sapiens | 100.0 | |
| CHEK2 | CHEK2 | Homo sapiens | 100.0 | |
| CLK1 | CLK1 | Homo sapiens | 100.0 | |
| CLK2 | CLK2 | Homo sapiens | 100.0 | |
| CLK3 | CLK3 | Homo sapiens | 100.0 | |
| CSNK1E | CSNK1E | Homo sapiens | 100.0 | |
| CSNK1G3 | CSNK1G3 | Homo sapiens | 100.0 | |
| CSNK2A1 | CSNK2A1 | Homo sapiens | 100.0 | |
| DAPK1 | DAPK1 | Homo sapiens | 100.0 | |
| DCAMKL1 | DCLK1 | Homo sapiens | 100.0 | |
| DCAMKL3 | DCLK3 | Homo sapiens | 100.0 | |
| DMPK | DMPK | Homo sapiens | 100.0 | |
| DYRK2 | DYRK2 | Homo sapiens | 100.0 | |
| EGFR | EGFR | Homo sapiens | 100.0 | |
| EPHA2 | EPHA2 | Homo sapiens | 100.0 | |
| EPHA8 | EPHA8 | Homo sapiens | 100.0 | |
| EPHB1 | EPHB1 | Homo sapiens | 100.0 | |
| EPHB2 | EPHB2 | Homo sapiens | 100.0 | |
| EPHB6 | EPHB6 | Homo sapiens | 100.0 | |
| ERBB2 | ERBB2 | Homo sapiens | 100.0 | |
| ERBB4 | ERBB4 | Homo sapiens | 100.0 | |
| ERK8 | MAPK15 | Homo sapiens | 100.0 | |
| ERN1 | ERN1 | Homo sapiens | 100.0 | |
| FER | FER | Homo sapiens | 100.0 | |
| FGFR2 | FGFR2 | Homo sapiens | 100.0 | |
| FGFR3 | FGFR3 | Homo sapiens | 100.0 | |
| GRK1 | GRK1 | Homo sapiens | 100.0 | |
| GRK2 | GRK2 | Homo sapiens | 100.0 | |
| GRK3 | GRK3 | Homo sapiens | 100.0 | |
| GSK3B | GSK3B | Homo sapiens | 100.0 | |
| HASPIN | HASPIN | Homo sapiens | 100.0 | |
| HCK | HCK | Homo sapiens | 100.0 | |
| HIPK2 | HIPK2 | Homo sapiens | 100.0 | |
| HIPK3 | HIPK3 | Homo sapiens | 100.0 | |
| IKK-alpha | CHUK | Homo sapiens | 100.0 | |
| IKK-beta | IKBKB | Homo sapiens | 100.0 | |
| IRAK1 | IRAK1 | Homo sapiens | 100.0 | |
| IRAK4 | IRAK4 | Homo sapiens | 100.0 | |
| ITK | ITK | Homo sapiens | 100.0 | |
| JAK1(JH2domain-pseudokinase) | JAK1 | Homo sapiens | 100.0 | |
| JAK2(JH1domain-catalytic) | JAK2 | Homo sapiens | 100.0 | |
| LATS2 | LATS2 | Homo sapiens | 100.0 | |
| LCK | LCK | Homo sapiens | 100.0 | |
| LKB1 | STK11 | Homo sapiens | 100.0 | |
| LRRK2 | LRRK2 | Homo sapiens | 100.0 | |
| LTK | LTK | Homo sapiens | 100.0 | |
| LYN | LYN | Homo sapiens | 100.0 | |
| MAP4K2 | MAP4K2 | Homo sapiens | 100.0 | |
| MAP4K3 | MAP4K3 | Homo sapiens | 100.0 | |
| MAPKAPK5 | MAPKAPK5 | Homo sapiens | 100.0 | |
| MARK4 | MARK4 | Homo sapiens | 100.0 | |
| MEK3 | MAP2K3 | Homo sapiens | 100.0 | |
| MKNK1 | MKNK1 | Homo sapiens | 100.0 | |
| MKNK2 | MKNK2 | Homo sapiens | 100.0 | |
| MLK3 | MAP3K11 | Homo sapiens | 100.0 | |
| MST1 | STK4 | Homo sapiens | 100.0 | |
| MST3 | STK24 | Homo sapiens | 100.0 | |
| MST4 | STK26 | Homo sapiens | 100.0 | |
| MTOR | MTOR | Homo sapiens | 100.0 | |
| MYLK | MYLK | Homo sapiens | 100.0 | |
| MYLK4 | MYLK4 | Homo sapiens | 100.0 | |
| MYO3A | MYO3A | Homo sapiens | 100.0 | |
| NEK10 | NEK10 | Homo sapiens | 100.0 | |
| NEK3 | NEK3 | Homo sapiens | 100.0 | |
| NIK | MAP3K14 | Homo sapiens | 100.0 | |
| OSR1 | OXSR1 | Homo sapiens | 100.0 | |
| p38-alpha | MAPK14 | Homo sapiens | 100.0 | |
| PAK1 | PAK1 | Homo sapiens | 100.0 | |
| PAK2 | PAK2 | Homo sapiens | 100.0 | |
| PCTK1 | CDK16 | Homo sapiens | 100.0 | |
| PDGFRA | PDGFRA | Homo sapiens | 100.0 | |
| PDPK1 | PDPK1 | Homo sapiens | 100.0 | |
| PHKG1 | PHKG1 | Homo sapiens | 100.0 | |
| PIK3C2B | PIK3C2B | Homo sapiens | 100.0 | |
| PIK3CA | PIK3CA | Homo sapiens | 100.0 | |
| PIK3CD | PIK3CD | Homo sapiens | 100.0 | |
| PIM1 | PIM1 | Homo sapiens | 100.0 | |
| PIM2 | PIM2 | Homo sapiens | 100.0 | |
| PIM3 | PIM3 | Homo sapiens | 100.0 | |
| PIP5K1C | PIP5K1C | Homo sapiens | 100.0 | |
| PIP5K2C | PIP4K2C | Homo sapiens | 100.0 | |
| PKAC-alpha | PRKACA | Homo sapiens | 100.0 | |
| PKAC-beta | PRKACB | Homo sapiens | 100.0 | |
| PKMYT1 | PKMYT1 | Homo sapiens | 100.0 | |
| PLK2 | PLK2 | Homo sapiens | 100.0 | |
| PLK3 | PLK3 | Homo sapiens | 100.0 | |
| PLK4 | PLK4 | Homo sapiens | 100.0 | |
| PRKCE | PRKCE | Homo sapiens | 100.0 | |
| PRKD1 | PRKD1 | Homo sapiens | 100.0 | |
| PRKD2 | PRKD2 | Homo sapiens | 100.0 | |
| PRKX | PRKX | Homo sapiens | 100.0 | |
| QSK | SIK3 | Homo sapiens | 100.0 | |
| RIOK2 | RIOK2 | Homo sapiens | 100.0 | |
| RIPK5 | DSTYK | Homo sapiens | 100.0 | |
| ROCK1 | ROCK1 | Homo sapiens | 100.0 | |
| ROCK2 | ROCK2 | Homo sapiens | 100.0 | |
| ROS1 | ROS1 | Homo sapiens | 100.0 | |
| RPS6KA4(Kin.Dom.2-C-terminal) | RPS6KA4 | Homo sapiens | 100.0 | |
| RPS6KA5(Kin.Dom.1-N-terminal) | RPS6KA5 | Homo sapiens | 100.0 | |
| RPS6KA5(Kin.Dom.2-C-terminal) | RPS6KA5 | Homo sapiens | 100.0 | |
| RSK1(Kin.Dom.2-C-terminal) | RPS6KA1 | Homo sapiens | 100.0 | |
| RSK2(Kin.Dom.1-N-terminal) | RPS6KA3 | Homo sapiens | 100.0 | |
| RSK3(Kin.Dom.2-C-terminal) | RPS6KA2 | Homo sapiens | 100.0 | |
| RSK4(Kin.Dom.1-N-terminal) | RPS6KA6 | Homo sapiens | 100.0 | |
| RSK4(Kin.Dom.2-C-terminal) | RPS6KA6 | Homo sapiens | 100.0 | |
| S6K1 | RPS6KB1 | Homo sapiens | 100.0 | |
| SBK1 | SBK1 | Homo sapiens | 100.0 | |
| SgK110 | SBK3 | Homo sapiens | 100.0 | |
| SGK2 | SGK2 | Homo sapiens | 100.0 | |
| SIK2 | SIK2 | Homo sapiens | 100.0 | |
| SLK | SLK | Homo sapiens | 100.0 | |
| SRC | SRC | Homo sapiens | 100.0 | |
| SRMS | SRMS | Homo sapiens | 100.0 | |
| STK33 | STK33 | Homo sapiens | 100.0 | |
| SYK | SYK | Homo sapiens | 100.0 | |
| TAK1 | MAP3K7 | Homo sapiens | 100.0 | |
| TAOK1 | TAOK1 | Homo sapiens | 100.0 | |
| TAOK2 | TAOK2 | Homo sapiens | 100.0 | |
| TAOK3 | TAOK3 | Homo sapiens | 100.0 | |
| TEC | TEC | Homo sapiens | 100.0 | |
| TGFBR2 | TGFBR2 | Homo sapiens | 100.0 | |
| TNIK | TNIK | Homo sapiens | 100.0 | |
| TNK2 | TNK2 | Homo sapiens | 100.0 | |
| TRKB | NTRK2 | Homo sapiens | 100.0 | |
| TSSK1B | TSSK1B | Homo sapiens | 100.0 | |
| TYK2(JH1domain-catalytic) | TYK2 | Homo sapiens | 100.0 | |
| TYK2(JH2domain-pseudokinase) | TYK2 | Homo sapiens | 100.0 | |
| ULK2 | ULK2 | Homo sapiens | 100.0 | |
| ULK3 | ULK3 | Homo sapiens | 100.0 | |
| VEGFR2 | KDR | Homo sapiens | 100.0 | |
| WEE1 | WEE1 | Homo sapiens | 100.0 | |
| YES | YES1 | Homo sapiens | 100.0 | |
| ZAP70 | ZAP70 | Homo sapiens | 100.0 |
BAY 1816032
The final concentration of BAY 1816032 was between 100 nM and 10 µM, and the final concentration of the solvent DMSO was 0.5%. After 4 days of continous incubation, the cells were fixed with glutaraldehyde, stained with crystal violet, and the absorbance was recorded at 595 nm. All measurements were done in quadruplicates. The values were normalized to the absorbance of solvent treated cells (=100%) and the absorbance of a reference plate which was fixed at the time point of compound application (=0%). Halfmaximal growth inhibition (IC50) was determined as compound concentration, which was required to achieve 50% inhibition of cellular growth using a 4-parameter fit. Shown are data from PMID: 30429199 (Supplementary Table 2) .
Conclusion: The average IC50 is 1.4 µM with a range from 0.47 to 5.3 µM. In the presence of 3 nM Paclitaxel the IC50 is 63 nM in HeLa cells.
| Tumor type | Cell line | Species | Cell Proliferation IC50 [µM] | Time [day] |
|---|---|---|---|---|
| Breast | MDA-MB-436 | Homo sapiens | 1.20 | 4 |
| Breast | MDA-MB-453 | Homo sapiens | 1.20 | 4 |
| Breast | MDA-MB-468 | Homo sapiens | 1.00 | 4 |
| Breast | SK-BR-3 | Homo sapiens | 1.10 | 4 |
| Breast | SUM-149 | Homo sapiens | 0.64 | 4 |
| Bladder | HT-1197 | Homo sapiens | 4.90 | 4 |
| Cervix | HeLa | Homo sapiens | 1.60 | 4 |
| Cervix | HeLa (presence of 3 nM Paclitaxel) | Homo sapiens | 0.06 | 4 |
| Cervix | HeLa-MaTu-ADR | Homo sapiens | 1.10 | 4 |
| Colon | Caco2 | Homo sapiens | 1.00 | 4 |
| Colon | HCT116 | Homo sapiens | 1.20 | 4 |
| Colon | Lovo | Homo sapiens | 0.70 | 4 |
| Colon | OUMS-23 | Homo sapiens | 2.60 | 4 |
| Mantle cell lymphoma | GRANTA-519 | Homo sapiens | 1.10 | 4 |
| Melanoma | A375 | Homo sapiens | 0.76 | 4 |
| Melanoma | HT-144 | Homo sapiens | 1.30 | 4 |
| Gastric | KATO III | Homo sapiens | 3.00 | 4 |
| Gastric | MKN-45 | Homo sapiens | 3.50 | 4 |
| Glioblastoma/ Neuroglioma | H4 | Homo sapiens | 0.93 | 4 |
| NSCLC | Calu-6 | Homo sapiens | 0.47 | 4 |
| NSCLC | NCI-H460 | Homo sapiens | 1.10 | 4 |
| NSCLC | NCI-H1299 | Homo sapiens | 2.40 | 4 |
| NSCLC | NCI-H1395 | Homo sapiens | 5.40 | 4 |
| NSCLC | NCI-H1437 | Homo sapiens | 2.80 | 4 |
| NSCLC | NCI-H1651 | Homo sapiens | 2.70 | 4 |
| NSCLC | NCI-H1703 | Homo sapiens | 0.92 | 4 |
| NSCLC | NCI-H1755 | Homo sapiens | 1.40 | 4 |
| NSCLC | NCI-H1792 | Homo sapiens | 1.60 | 4 |
| NSCLC | NCI-H1838 | Homo sapiens | 2.90 | 4 |
| NSCLC | NCI-H1944 | Homo sapiens | 3.00 | 4 |
| NSCLC | NCI-H2009 | Homo sapiens | 2.10 | 4 |
| NSCLC | NCI-H2087 | Homo sapiens | 0.87 | 4 |
| NSCLC | NCI-H2228 | Homo sapiens | 1.90 | 4 |
| NSCLC | NCI-H23 | Homo sapiens | 1.00 | 4 |
| NSCLC | NCI-H2347 | Homo sapiens | 5.80 | 4 |
| Ovary | Colo-704 | Homo sapiens | 1.00 | 4 |
| Ovary | SK-OV-3 | Homo sapiens | 2.20 | 4 |
| Pancreas | MIA Paca-2 | Homo sapiens | 3.00 | 4 |
| Pancreas | Panc-1 | Homo sapiens | 3.30 | 4 |
| Prostate | DU145 | Homo sapiens | 1.10 | 4 |
| Prostate | PC-3 | Homo sapiens | 3.40 | 4 |
| Prostate | 22RV1 | Homo sapiens | 0.71 | 4 |
| Skin | A431 | Homo sapiens | 3.00 | 4 |
| Mouse melanoma | B16F10 | Mus musculus | 2.00 | 4 |