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Selectivity data for probe TP-051 and control TP-051n


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TP-051


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1A HTR1A 1.37
5-HT1E HTR1E 3.83
5-HT2A HTR2A 7.36
5-HT2B HTR2B 21.48
5-HT2C HTR2C 14.08
5-HT3 HTR3A 6.06
5-HT5A HTR5A 13.33
5-HT6 HTR6 -7.86
5-HT7A HTR7 2.66
Alpha1A ADRA1A -19.46
Alpha1B ADRA1B 0.86
Alpha1D ADRA1D 50.81 7519.69 5.12
Alpha2A ADRA2A 13.03
Alpha2B ADRA2B 13.10
Alpha2C ADRA2C 5.47
Beta1 ADRB1 14.41
Beta2 ADRB2 -36.94 > 10000.00 < 5.00
GABAA/BZP 23.68
D1 DRD1 13.71
D2 DRD2 16.59
D3 DRD3 59.59 924.70 6.03
D4 DRD4 85.41 1225.46 5.91
D5 DRD5 32.24
DAT SLC6A3 53.67 > 10000.00 < 5.00
DOR OPRD1 -12.09
H1 HRH1 12.01
H3 HRH3 21.10
H4 HRH4 10.80
KOR OPRK1 10.17
M1 CHRM1 15.85
M2 CHRM2 2.31
M3 CHRM3 -0.18
M4 CHRM4 -16.38
M5 CHRM5 20.38
MOR OPRM1 1.32
NET SLC6A2 19.13
GABA/PBR -0.04
SERT SLC6A4 -27.60
Sigma 1 SIGMAR1 8.90
Sigma 2 TMEM97 19.61
5-HT1B HTR1B 19.32
5-HT1D HTR1D 35.77
Beta3 ADRB3 -5.43
H2 HRH2 5.95

TP-051n


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1A HTR1A -6.09
5-HT1E HTR1E -1.42
5-HT2A HTR2A -10.88
5-HT2B HTR2B 3.00
5-HT2C HTR2C -12.10
5-HT3 HTR3A -5.96
5-HT5A HTR5A -24.79
5-HT6 HTR6 -22.62
5-HT7A HTR7 -19.11
Alpha1A ADRA1A -29.11
Alpha1B ADRA1B -18.88
Alpha1D ADRA1D -27.43
Alpha2A ADRA2A 13.08
Alpha2B ADRA2B -0.21
Alpha2C ADRA2C -4.04
Beta1 ADRB1 -0.49
Beta2 ADRB2 -17.64
GABAA/BZP 19.51
D1 DRD1 20.90
D2 DRD2 8.60
D3 DRD3 7.34
D4 DRD4 7.27
D5 DRD5 17.53
DAT SLC6A3 42.25
DOR OPRD1 -7.07
H1 HRH1 -2.18
H3 HRH3 6.70
H4 HRH4 17.43
KOR OPRK1 4.04
M1 CHRM1 -1.50
M2 CHRM2 -24.00
M3 CHRM3 -16.32
M4 CHRM4 -4.72
M5 CHRM5 -4.74
MOR OPRM1 -7.84
NET SLC6A2 -18.15
GABA/PBR -94.26 2752.33 5.56
SERT SLC6A4 -11.14
Sigma 1 SIGMAR1 16.71
Sigma 2 TMEM97 1.49
5-HT1B HTR1B 23.18
5-HT1D HTR1D 29.53
Beta3 ADRB3 6.71
H2 HRH2 7.66

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TP-051

Results are significant for > 50 % inhibition.

Conclusion: Closest off-target is TBXA2R with 60 % inhibition.

Target protein HGNC name Species Cmp. conc. % inhibition Reference compound name Reference compound IC50 [nM] Assay ID
Adenosine A1 ADORA1 Homo sapiens 10 µM -1.0 R(-)-PIA 830.00 200510
Adenosine A2A ADORA2A Homo sapiens 10 µM 5.0 CGS-21680 130.00 200610
Adenosine A3 ADORA3 Homo sapiens 10 µM 5.0 IB-MECA 0.78 200720
Adrenergic α1, Non-selective Rattus sp. 10 µM -2.0 203500
Adrenergic α2, Non-selective Rattus sp. 10 µM 8.0 203900
Adrenergic beta1 ADRB1 Homo sapiens 10 µM 5.0 S(-)-Propranolol 2.50 204010
Adrenergic beta2 ADRB2 Homo sapiens 10 µM 3.0 S(-)-Propranolol 0.78 204110
Adrenergic beta3 ADRB3 Homo sapiens 10 µM 15.0 Alprenolol 180.00 204200
Angiotensin AT1 AGTR1 Homo sapiens 10 µM 14.0 Saralasin 0.64 210020
Angiotensin AT2 AGTR2 Homo sapiens 10 µM -4.0 Saralasin 0.28 210110
Bradykinin B1 BDKRB1 Homo sapiens 10 µM 14.0 (Des-Arg10)-Kallidin 0.87 212510
Bradykinin B2 BDKRB2 Homo sapiens 10 µM 7.0 Bradykinin 0.89 212610
Calcium Channel L-Type, Benzothiazepine CACNA1C Rattus sp. 10 µM -3.0 Diltiazem 0.04 214510
Calcium Channel L-Type, Dihydropyridine CACNA1C Rattus sp. 10 µM 7.0 Nitrendipine 0.72 214600
Calcium Channel L-Type, Phenylalkylamine CACNA1C Rattus sp. 10 µM 3.0 Methoxyverapamil (D-600) 22.00 215000
Calcium Channel N-Type CACNA1B Rattus sp. 10 µM -4.0 ω-Conotoxin GVIA 0.03 216000
Cannabinoid CB1 CNR1 Homo sapiens 10 µM 8.0 217010
Chemokine CXCR1/2 (IL-8, Non-selective) Homo sapiens 10 µM 3.0 244300
Cholecystokinin CCK1 (CCKA) CCKAR Homo sapiens 10 µM 4.0 218010
Cholecystokinin CCK2 (CCKB) CCKBR Homo sapiens 10 µM -16.0 Sincalide 0.14 218120
Dopamine D1 DRD1 Homo sapiens 10 µM 24.0 R(+)-SCH-23390 1.40 219500
Dopamine D2L DRD2 Homo sapiens 10 µM -2.0 Spiperone 0.26 219600
Dopamine D3 DRD3 Homo sapiens 10 µM -7.0 Spiperone 0.36 219800
Dopamine D4.2 DRD4 Homo sapiens 10 µM 9.0 Spiperone 29.00 219900
Endothelin ETA EDNRA Homo sapiens 10 µM -2.0 Endothelin-1 0.23 224010
Endothelin ETB EDNRB Homo sapiens 10 µM 0.0 Endothelin-1 0.13 224110
Estrogen ERalpha ESR1 Homo sapiens 10 µM 3.0 Diethylstilbestrol 0.77 226010
Estrogen ERbeta ESR2 Homo sapiens 10 µM 20.0 Diethylstilbestrol 0.61 226050
GABAA, Agonist Site Rattus sp. 10 µM 3.0 4-aminobutyric acid 0.03 226500
GABAA, Benzodiazepine, Central Rattus sp. 10 µM -12.0 Hydrogen diazepam chloride 0.02 226600
GABAA, Chloride Channel, TBOB Rattus sp. 10 µM 21.0 Picrotoxin 270.00 226810
GABAB1B GABBR1 Homo sapiens 10 µM 1.0 228700
GABAB1A GABBR1 Homo sapiens 10 µM 7.0 228600
Glucocorticoid NR3C1 Homo sapiens 10 µM 0.0 232010
Glutamate, AMPA Rattus sp. 10 µM 4.0 L-Glutamic acid 320.00 232600
Glutamate, Kainate GRIK2 Rattus sp. 10 µM -10.0 232700
Glutamate, NMDA, Glycine Rattus sp. 10 µM 8.0 MDL 105,519 22.00 232910
Glutamate, NMDA, Phencyclidine Rattus sp. 10 µM -4.0 Dizolcipine ((+)-MK-801) 5.10 233000
Glycine, Strychnine-Sensitive Rattus sp. 10 µM 7.0 (-)-Strychnine 8.90 239000
Growth Hormone Secretagogue (GHS, Ghrelin) GHSR Homo sapiens 10 µM 2.0 Ghrelin (human) 0.13 239300
Histamine H1 HRH1 Homo sapiens 10 µM -7.0 Pyrilamine 3.30 239610
Histamine H2 HRH2 Homo sapiens 10 µM 26.0 Tiotidine 22.00 239710
Imidazoline I2, Central Rattus sp. 10 µM -7.0 Idazoxan 12.00 241000
Insulin INSR Rattus sp. 10 µM 7.0 Insulin 6.10 243000
Muscarinic M1 CHRM1 Homo sapiens 10 µM -9.0 252600
Muscarinic M2 CHRM2 Homo sapiens 10 µM 4.0 252700
Muscarinic M3 CHRM3 Homo sapiens 10 µM 4.0 252800
Nicotinic Acetylcholine Homo sapiens 10 µM -14.0 Epibatidine 0.08 258590
Opiate µ (OP3, MOP) OPRM1 Homo sapiens 10 µM 5.0 DAMGO 20.00 260410
Opiate, Non-Selective Rattus sp. 10 µM -8.0 Naloxone 0.00 260500
Phorbol Ester Mus musculus 10 µM -9.0 Phorbol myristate acetate 0.79 264500
Platelet Activating Factor (PAF) PTAFR Homo sapiens 10 µM 4.0 PAF 0.28 265010
Potassium Channel [KATP] KCNJ11 Cricetinae 10 µM 19.0 Glyburide 5.70 265600
Potassium Channel [SKCA] Rattus sp. 10 µM -5.0 24345-16-2 265800
Progesterone PR-B PGR Homo sapiens 10 µM 10.0 Progesterone 1.50 268020
Prostanoid, Thromboxane A2 (TP) TBXA2R Homo sapiens 10 µM 60.0 ICI-19Z,605 2.10 285510
Serotonin (5-Hydroxytryptamine) 5-HT1, Non-Selective Rattus sp. 10 µM 16.0 Serotonin (5-HT) 1.10 271000
Serotonin (5-Hydroxytryptamine) 5-HT2, Non-Selective Rattus sp. 10 µM -15.0 Ketanserin 271600
Serotonin (5-Hydroxytryptamine) 5-HT3 HTR3A Homo sapiens 10 µM -3.0 MDL-72222 11.00 271910
Serotonin (5-Hydroxytryptamine) 5-HT4 HTR4 Cavia porcellus 10 µM 8.0 CHEMBL83954 272000
Sodium Channel, Site 2 Rattus sp. 10 µM 6.0 Dibucaine 61.00 279510
Somatostatin sst2 SSTR2 Homo sapiens 10 µM 5.0 Somatostatin-14 0.01 282700
Tachykinin NK1 TACR1 Homo sapiens 10 µM 17.0 L-703,606 25.00 255510
Tachykinin NK2 TACR2 Homo sapiens 10 µM 29.0 MEN-10,376 110.00 255600
Tachykinin NK3 TACR3 Homo sapiens 10 µM 30.0 255700
Testosterone AR Rattus sp. 10 µM 17.0 285010
Transporter, Dopamine (DAT) SLC6A3 Homo sapiens 10 µM 5.0 GBR-12909 1.70 220320
Transporter, GABA Rattus sp. 10 µM -4.0 NO-711 200.00 226400
Transporter, Norepinephrine (NET) SLC6A2 Homo sapiens 10 µM 22.0 Desipramine 0.93 204410
Transporter, Serotonin (5- Hydroxytryptamine) (SERT) SLC6A4 Homo sapiens 10 µM -5.0 274020
Vasopressin V1A AVPR1A Homo sapiens 10 µM 0.0 287520
Vasopressin V1B AVPR1B Homo sapiens 10 µM -4.0 (Arg8)-Vasopressin 0.66 287560
Vasopressin V2 AVPR2 Homo sapiens 10 µM 0.0 (Arg8)-Vasopressin 4.50 287610
 

TP-051n

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 -4.0 R(-)-PIA 830.0 200510
Adenosine A2A ADORA2A Homo sapiens 10 µM 10.0 CGS-21680 130.0 200610
Adenosine A3 ADORA3 Homo sapiens 10 µM 0.0 IB-MECA 0.8 200720
Adrenergic α1, Non-selective Rattus sp. 10 µM -1.0 203500
Adrenergic α2, Non-selective Rattus sp. 10 µM 6.0 203900
Adrenergic beta1 ADRB1 Homo sapiens 10 µM -4.0 S(-)-Propranolol 2.5 204010
Adrenergic beta2 ADRB2 Homo sapiens 10 µM -7.0 S(-)-Propranolol 0.8 204110
Adrenergic beta3 ADRB3 Homo sapiens 10 µM -3.0 Alprenolol 180.0 204200
Anaphylatoxin C5a C5AR1 Homo sapiens 10 µM -1.0
Angiotensin AT1 AGTR1 Homo sapiens 10 µM 1.0 Saralasin 0.6 210020
Angiotensin AT2 AGTR2 Homo sapiens 10 µM 1.0 Saralasin 0.3 210110
Bradykinin B1 BDKRB1 Homo sapiens 10 µM 19.0 (Des-Arg10)-Kallidin 0.9 212510
Bradykinin B2 BDKRB2 Homo sapiens 10 µM -4.0 Bradykinin 0.9 212610
Calcium Channel L-Type, Benzothiazepine CACNA1C Rattus sp. 10 µM 5.0 Diltiazem 0.0 214510
Calcium Channel L-Type, Dihydropyridine CACNA1C Rattus sp. 10 µM -3.0 Nitrendipine 0.7 214600
Calcium Channel L-Type, Phenylalkylamine CACNA1C Rattus sp. 10 µM -1.0 Methoxyverapamil (D-600) 22.0 215000
Calcium Channel N-Type CACNA1B Rattus sp. 10 µM -9.0 ω-Conotoxin GVIA 0.0 216000
Cannabinoid CB1 CNR1 Homo sapiens 10 µM -6.0 R(+)-WIN-55,212-2 12.0 217020
Chemokine CXCR1/2 (IL-8, Non-selective) Homo sapiens 10 µM 4.0
Cholecystokinin CCK1 (CCKA) CCKAR Homo sapiens 10 µM -9.0
Cholecystokinin CCK2 (CCKB) CCKBR Homo sapiens 10 µM 5.0 Sincalide 0.1 218120
Dopamine D1 DRD1 Homo sapiens 10 µM -3.0 R(+)-SCH-23390 1.4 219500
Dopamine D2L DRD2 Homo sapiens 10 µM -4.0 Spiperone 0.3 219600
Dopamine D3 DRD3 Homo sapiens 10 µM 4.0 Spiperone 0.4 219800
Dopamine D4.2 DRD4 Homo sapiens 10 µM 6.0 Spiperone 29.0 219900
Endothelin ETA EDNRA Homo sapiens 10 µM -2.0 Endothelin-1 0.2 224010
Endothelin ETB EDNRB Homo sapiens 10 µM 15.0 Endothelin-1 0.1 224110
Estrogen ERalpha ESR1 Homo sapiens 10 µM 7.0 Diethylstilbestrol 0.8 226010
Estrogen ERbeta ESR2 Homo sapiens 10 µM 8.0 Diethylstilbestrol 0.6 226050
GABAA, Agonist Site Rattus sp. 10 µM 8.0 4-aminobutyric acid 0.0 226500
GABAA, Benzodiazepine, Central Rattus sp. 10 µM -1.0 Hydrogen diazepam chloride 0.0 226600
GABAA, Chloride Channel, TBOB Rattus sp. 10 µM 14.0 Picrotoxin 270.0 226810
GABAB1B GABBR1 Homo sapiens 10 µM 10.0
GABAB1A GABBR1 Homo sapiens 10 µM 20.0
Glucocorticoid NR3C1 Homo sapiens 10 µM 14.0
Glutamate, AMPA Rattus sp. 10 µM -3.0 L-Glutamic acid 320.0 232600
Glutamate, Kainate GRIK2 Rattus sp. 10 µM 8.0 232700
Glutamate, NMDA, Glycine Rattus sp. 10 µM 7.0 MDL 105,519 22.0 232910
Glutamate, NMDA, Phencyclidine Rattus sp. 10 µM 5.0 Dizolcipine ((+)-MK-801) 5.1 233000
Glycine, Strychnine-Sensitive Rattus sp. 10 µM 5.0 (-)-Strychnine 8.9 239000
Growth Hormone Secretagogue (GHS, Ghrelin) GHSR Homo sapiens 10 µM -1.0 Ghrelin (human) 0.1 239300
Histamine H1 HRH1 Homo sapiens 10 µM 2.0 Pyrilamine 3.3 239610
Histamine H2 HRH2 Homo sapiens 10 µM 2.0 Tiotidine 22.0 239710
Imidazoline I2, Central Rattus sp. 10 µM 3.0 Idazoxan 12.0 241000
Insulin INSR Rattus sp. 10 µM 0.0 Insulin 6.1 243000
Muscarinic M1 CHRM1 Homo sapiens 10 µM -7.0
Muscarinic M2 CHRM2 Homo sapiens 10 µM -3.0
Muscarinic M3 CHRM3 Homo sapiens 10 µM 1.0
Nicotinic Acetylcholine Homo sapiens 10 µM -5.0 Epibatidine 0.1 258590
Opiate µ (OP3, MOP) OPRM1 Homo sapiens 10 µM 10.0 DAMGO 20.0 260410
Opiate, Non-Selective Rattus sp. 10 µM 3.0 Naloxone 0.0 260500
Phorbol Ester Mus musculus 10 µM -3.0 Phorbol myristate acetate 0.8 264500
Platelet Activating Factor (PAF) PTAFR Homo sapiens 10 µM 2.0 PAF 0.3 265010
Potassium Channel [KATP] KCNJ11 Cricetinae 10 µM -3.0 Glyburide 5.7 265600
Potassium Channel [SKCA] Rattus sp. 10 µM 1.0 24345-16-2 265800
Progesterone PR-B PGR Homo sapiens 10 µM 6.0 Progesterone 1.5 268020
Prostanoid, Thromboxane A2 (TP) TBXA2R Homo sapiens 10 µM 28.0 ICI-19Z,605 2.1 285510
Serotonin (5-Hydroxytryptamine) 5-HT1, Non-Selective Rattus sp. 10 µM -9.0 Serotonin (5-HT) 1.1 271000
Serotonin (5-Hydroxytryptamine) 5-HT2, Non-Selective Rattus sp. 10 µM -3.0 Ketanserin 271600
Serotonin (5-Hydroxytryptamine) 5-HT3 HTR3A Homo sapiens 10 µM -11.0 MDL-72222 11.0 271910
Serotonin (5-Hydroxytryptamine) 5-HT4 HTR4 Cavia porcellus 10 µM -8.0 CHEMBL83954 272000
Sodium Channel, Site 2 Rattus sp. 10 µM -5.0 Dibucaine 61.0 279510
Somatostatin sst2 SSTR2 Homo sapiens 10 µM -6.0 Somatostatin-14 0.0 282700
Tachykinin NK1 TACR1 Homo sapiens 10 µM 3.0 L-703,606 25.0 255510
Tachykinin NK2 TACR2 Homo sapiens 10 µM 3.0 MEN-10,376 110.0 255600
Tachykinin NK3 TACR3 Homo sapiens 10 µM 10.0 255710
Testosterone AR Rattus sp. 10 µM 26.0 285010
Transporter, Dopamine (DAT) SLC6A3 Homo sapiens 10 µM -8.0 GBR-12909 1.7 220320
Transporter, GABA Rattus sp. 10 µM 7.0 NO-711 200.0 226400
Transporter, Norepinephrine (NET) SLC6A2 Homo sapiens 10 µM 5.0 Desipramine 0.9 204410
Transporter, Serotonin (5- Hydroxytryptamine) (SERT) SLC6A4 Homo sapiens 10 µM 2.0 Fluoxetine 8.6 274030
Vasopressin V1A AVPR1A Homo sapiens 10 µM -4.0 287520
Vasopressin V1B AVPR1B Homo sapiens 10 µM -4.0 (Arg8)-Vasopressin 0.7 287560
Vasopressin V2 AVPR2 Homo sapiens 10 µM -23.0 (Arg8)-Vasopressin 4.5 287610

TP-051

Results are significant for > 50 % inhibition.

Conclusion: Closest off-targets [% inhibition] are ALOX5 (85 %), EGFR (61 %), MAPK14 (60 %) and TBXAS1 (64 %)

Target protein HGNC name Species Cmp. conc. % inhibition Reference compound name Reference compound IC50 [µM] Assay ID
Cholinesterase, Acetyl, ACES ACHE Homo sapiens 10 µM -15.0 Physostigmine 0.12 104010
ATPase, Ca2+ Rattus sp. 10 µM -1.0 107490
ATPase, Na+/K+ Canis lupus familiaris 10 µM 4.0 107700
Carbonic Anhydrase Homo sapiens 10 µM 27.0 112000
Cyclooxygenase COX-1 PTGS1 Homo sapiens 10 µM 14.0 Indomethacin 0.04 116020
Cyclooxygenase COX-2 PTGS2 Homo sapiens 10 µM -5.0 Rofecoxib 0.17 118010
HMG-CoA Reductase HMGCR Rattus sp. 10 µM -5.0 124000
Lipoxygenase 5-LO ALOX5 Homo sapiens 10 µM 85.0 NDGA 0.13 136010
Monoamine Oxidase MAO-A MAOA Homo sapiens 10 µM 7.0 Clorgyline 0.00 140010
Monoamine Oxidase MAO-B MAOB Homo sapiens 10 µM 6.0 R(-)-Deprenyl 0.01 140120
Nitric Oxide Synthase, Inducible (iNOS) NOS2 Mus musculus 10 µM -4.0 S-Methylisothiourea 2.30 144000
Nitric Oxide Synthase, Neuronal (nNOS) NOS1 Rattus sp. 10 µM -7.0 S-methylisothiourea 142000
Peptidase, Angiotensin Converting Enzyme ACE Oryctolagus cuniculus 10 µM 20.0 Captopril 0.01 107300
Peptidase, CTSG (Cathepsin G) CTSG Homo sapiens 10 µM 20.0 Chymostatin 2.10 112510
Peptidase, Factor VIIa F7 Homo sapiens 10 µM -10.0 UNII-N62UL02WW4 0.71 113500
Peptidase, Factor Xa F10 Homo sapiens 10 µM 2.0 UNII-N62UL02WW4 0.28 113600
Peptidase, Matrix Metalloproteinase-1 (MMP-1) MMP1 Homo sapiens 10 µM 2.0 TIMP-2 0.01 114110
Peptidase, Matrix Metalloproteinase-7 (MMP-7) MMP7 Homo sapiens 10 µM 1.0 GM-6001 114710
Peptidase, Matrix Metalloproteinase-13 (MMP-13) MMP13 Homo sapiens 10 µM 5.0 GM-6001 115300
Peptidase, Matrix Metalloproteinase-14 (MMP-14) MMP14 Homo sapiens 10 µM 3.0 GM-6001 115400
Peptidase, Metalloproteinase, Neutral Endopeptidase MME Homo sapiens 10 µM 4.0 Phosphoramidon 0.01 164000
Peptidase, Renin REN Homo sapiens 10 µM -1.0 164600
Peptidase, Thrombin F2 Homo sapiens 10 µM -1.0 UNII-N62UL02WW4 0.00 165000
Peptidase, Tumor Necrosis Factor-alpha Converting Enzyme (TACE) ADAM17 Homo sapiens 10 µM 36.0 Ilomastat 0.02 166500
Phosphodiesterase PDE3 Homo sapiens 10 µM 3.0 Cilostamide 0.05 152000
Phosphodiesterase PDE4 Homo sapiens 10 µM 26.0 Ro 20-1724 1.10 154000
Phosphodiesterase PDE5 PDE5A Homo sapiens 10 µM -6.0 Zaprinast 156000
Phosphodiesterase PDE6 Bos taurus 10 µM 20.0 Zaprinast 156100
Phospholipase PLA2-I Sus scrofa 10 µM 6.0 Quinacrine 130.00 160000
Protein Serine/Threonine Kinase, Ca2+/Calmodulin-Dep.II Rattus sp. 10 µM 44.0 168000
Protein Serine/Threonine Kinase, cdk1/Cyclin B Homo sapiens 10 µM 14.0 168100
Protein Serine/Threonine Kinase, MAPK3 (ERK1) MAPK3 Homo sapiens 10 µM 30.0 Staurosporine 1.60 171000
Protein Serine/Threonine Kinase, GSK-3β GSK3B Homo sapiens 10 µM 19.0 5-iodo-Indirubin-3'-monoxime 0.00 176500
Protein Serine/Threonine Kinase, MAPK14 (p38α) MAPK14 Homo sapiens 10 µM 60.0 SB-Z0Z190 0.02 176600
Protein Serine/Threonine Kinase, PKA, Non-Selective Bos taurus 10 µM 5.0 H-7 3.60 177000
Protein Serine/Threonine Kinase, PKBα/Akt1 AKT1 Homo sapiens 10 µM -1.0 177500
Protein Serine/Threonine Kinase, PKC, Non-Selective Rattus sp. 10 µM -8.0 Staurosporine 0.00 178010
Protein Serine/Threonine Phosphatase, Calcineurin, PP2B PPP3CA Homo sapiens 10 µM 10.0 188010
Protein Tyrosine Kinase, EGF Receptor EGFR Homo sapiens 10 µM 61.0 Tyrphostin 47 1.10 170010
Protein Tyrosine Kinase, ERBB2 (HER2) ERBB2 Homo sapiens 10 µM -9.0 174000
Protein Tyrosine Kinase, Insulin Receptor INSR Homo sapiens 10 µM -13.0 Tyrphostin 47 3.10 175000
Protein Tyrosine Kinase, pp60 c-SRC SRC Homo sapiens 10 µM 1.0 Staurosporine 0.23 176800
Steroid 5α-Reductase Rattus sp. 10 µM 19.0 Finasteride 0.06 193600
Thromboxane Synthase TBXAS1 Homo sapiens 10 µM 64.0 194010
Xanthine Oxidase XDH Bos taurus 10 µM 1.0 Allopurinol 2.40 198000
 

TP-051n

Conclusion: Closest off-targets [% inhibition] are LYN (70 %), MAPK14 (66 %) and PKC (-114 %)

Target protein HGNC name Species Cmp. conc. % inhibition Reference compound name Reference compound IC50 [µM] Assay ID
Cholinesterase, Acetyl, ACES ACHE Homo sapiens 10 µM -4.0 Physostigmine 0.1 104010
ATPase, Ca2+, skeletal muscle Sus scrofa 10 µM -2.0 Cyclopiazonic acid 0.1 107480
ATPase, Na+/K+, heart Sus scrofa 10 µM -1.0 Ouabain 2.0 107710
Carbonic Anhydrase Homo sapiens 10 µM 11.0
Cyclooxygenase COX-1 PTGS1 Homo sapiens 10 µM -1.0 Indomethacin 0.0 116020
Cyclooxygenase COX-2 PTGS2 Homo sapiens 10 µM 17.0 Rofecoxib 0.2 118010
HMG-CoA Reductase HMGCR Rattus sp. 10 µM -21.0
Lipoxygenase 5-LO ALOX5 Homo sapiens 10 µM 24.0 NDGA 0.1 136010
Monoamine Oxidase MAO-A MAOA Homo sapiens 10 µM 33.0 Clorgyline 0.0 140010
Monoamine Oxidase MAO-B MAOB Homo sapiens 10 µM 9.0 R(-)-Deprenyl 0.0 140120
Nitric Oxide Synthase, Inducible (iNOS) NOS2 Mus musculus 10 µM -3.0 S-Methylisothiourea 2.3 144000
Nitric Oxide Synthase, Neuronal (nNOS) NOS1 Rattus sp. 10 µM 4.0 S-methylisothiourea 142000
Peptidase, Angiotensin Converting Enzyme ACE Oryctolagus cuniculus 10 µM -5.0 Captopril 0.0 107300
Peptidase, CTSG (Cathepsin G) CTSG Homo sapiens 10 µM 11.0 Chymostatin 2.1 112510
Peptidase, Factor VIIa F7 Homo sapiens 10 µM 6.0 UNII-N62UL02WW4 0.7 113500
Peptidase, Factor Xa F10 Homo sapiens 10 µM -1.0 UNII-N62UL02WW4 0.3 113600
Peptidase, Matrix Metalloproteinase-1 (MMP-1) MMP1 Homo sapiens 10 µM 3.0 TIMP-2 0.0 114110
Peptidase, Matrix Metalloproteinase-7 (MMP-7) MMP7 Homo sapiens 10 µM 3.0 GM-6001 114710
Peptidase, Matrix Metalloproteinase-13 (MMP-13) MMP13 Homo sapiens 10 µM 3.0 GM-6001 115300
Peptidase, Matrix Metalloproteinase-14 (MMP-14) MMP14 Homo sapiens 10 µM 5.0 GM-6001 115400
Peptidase, Metalloproteinase, Neutral Endopeptidase MME Homo sapiens 10 µM 5.0 Phosphoramidon 0.0 164000
Peptidase, Renin REN Homo sapiens 10 µM -10.0 164600
Peptidase, Thrombin F2 Homo sapiens 10 µM 5.0 UNII-N62UL02WW4 0.0 165000
Peptidase, Tumor Necrosis Factor-alpha Converting Enzyme (TACE) ADAM17 Homo sapiens 10 µM 22.0 Ilomastat 0.0 166500
Phosphodiesterase PDE3 Homo sapiens 10 µM 12.0 Cilostamide 0.1 152000
Phosphodiesterase PDE4 Homo sapiens 10 µM 11.0 Ro 20-1724 1.1 154000
Phosphodiesterase PDE5 PDE5A Homo sapiens 10 µM 12.0 Zaprinast 156000
Phosphodiesterase PDE6 Bos taurus 10 µM 15.0 Zaprinast 156100
Phospholipase PLA2-I Sus scrofa 10 µM -2.0 Quinacrine 130.0 160000
Protein Serine/Threonine Kinase, Ca2+/Calmodulin-Dep.II Rattus sp. 10 µM 20.0
Protein Serine/Threonine Kinase, ERK2 MAPK1 Mus musculus 10 µM 9.0
Protein Serine/Threonine Kinase, cdk1/Cyclin B Homo sapiens 10 µM -10.0
Protein Serine/Threonine Kinase, MAPK3 (ERK1) MAPK3 Homo sapiens 10 µM 23.0 Staurosporine 1.6 171000
Protein Serine/Threonine Kinase, MEK1 MAP2K1 Homo sapiens 11 µM 16.0
Protein Serine/Threonine Kinase, GSK-3β GSK3B Homo sapiens 10 µM 29.0 5-iodo-Indirubin-3'-monoxime 0.0 176500
Protein Serine/Threonine Kinase, IKK-1 CHUK Homo sapiens 10 µM 31.0 Staurosporine 0.1 176200
Protein Serine/Threonine Kinase, JNK1α1 MAPK8 Homo sapiens 10 µM 11.0
Protein Serine/Threonine Kinase, MAPK14 (p38α) MAPK14 Homo sapiens 10 µM 66.0 SB-Z0Z190 0.0 176600
Protein Serine/Threonine Kinase, PKA, Non-Selective Bos taurus 10 µM 14.0 H-7 3.6 177000
Protein Serine/Threonine Kinase, PKBα/Akt1 AKT1 Homo sapiens 10 µM -20.0
Protein Serine/Threonine Kinase, PKC, Non-Selective Rattus sp. 10 µM -114.0 Staurosporine 0.0 178010
Protein Serine/Threonine Phosphatase, Calcineurin, PP2B PPP3CA Homo sapiens 10 µM 0.0
Protein Tyrosine Kinase, EGF Receptor EGFR Homo sapiens 10 µM 3.0 Tyrphostin 47 1.1 170010
Protein Tyrosine Kinase, ERBB2 (HER2) ERBB2 Homo sapiens 10 µM 30.0
Protein Tyrosine Kinase, Fes FES Homo sapiens 10 µM 25.0
Protein Tyrosine Kinase, Insulin Receptor INSR Homo sapiens 10 µM -10.0 Tyrphostin 47 3.1 175000
Protein Tyrosine Kinase, Lyn B LYN Homo sapiens 10 µM 70.0
Protein Tyrosine Kinase, SRC SRC Homo sapiens 10 µM 0.0 Staurosporine 0.2 176800
Steroid 5α-Reductase Rattus sp. 10 µM 21.0 Finasteride 0.1 193600
Thromboxane Synthase TBXAS1 Homo sapiens 10 µM 13.0 1-(7-Carboxyheptyl)-Imidazole 0.0 194020
Xanthine Oxidase XDH Bos taurus 10 µM 24.0 Allopurinol 2.4 198000