BAY-1797 [Ligand Id: 12567] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4521594 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of Alpha2B | B | 5.37 | pKi | 4315.19 | nM | Ki | Data for DCP probe BAY-1797 |
| ChEMBL | GPCRScan assay: inhibition of Alpha2B | B | 5.37 | pKi | 4285.88 | nM | Ki | Data for DCP probe BAY-1797 |
| carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918] | ||||||||
| ChEMBL | Inhibition of carbonic anhydrase 2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2019) 62: 11194-11217 [PMID:31746599] |
| DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| ChEMBL | Antagonist activity at human DAT receptor by scintillation counting method | B | 5.66 | pIC50 | 2170 | nM | IC50 | J Med Chem (2019) 62: 11194-11217 [PMID:31746599] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2019) 62: 11194-11217 [PMID:31746599] |
| P2X1/P2X purinoceptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2094] [GtoPdb: 478] [UniProtKB: P51575] | ||||||||
| ChEMBL | Antagonist activity at human P2X1 receptor | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2019) 62: 11194-11217 [PMID:31746599] |
| P2X2/P2X purinoceptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2531] [GtoPdb: 479] [UniProtKB: Q9UBL9] | ||||||||
| ChEMBL | Antagonist activity at human P2X2 receptor | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2019) 62: 11194-11217 [PMID:31746599] |
| P2X3/P2X purinoceptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2998] [GtoPdb: 480] [UniProtKB: P56373] | ||||||||
| ChEMBL | Antagonist activity at human P2X3 receptor | B | 5.08 | pIC50 | 8300 | nM | IC50 | J Med Chem (2019) 62: 11194-11217 [PMID:31746599] |
| P2X4/P2X purinoceptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2104] [GtoPdb: 481] [UniProtKB: Q99571] | ||||||||
| ChEMBL | Ephys Qpatch Assay with 1321 N1 Astrocytoma cells | B | 6.49 | pIC50 | 320 | nM | IC50 | Data for DCP probe BAY-1797 |
| ChEMBL | Antagonist activity at human P2X4 receptor tranfected in human 1321N1 cells assessed as inhibition of inhibition of ATP-evoked current at -90 mV holding potential by Qpatch method | B | 6.49 | pIC50 | 320 | nM | IC50 | J Med Chem (2019) 62: 11194-11217 [PMID:31746599] |
| ChEMBL | Ephys Qpatch Assay with HEK293 cells | B | 6.56 | pIC50 | 274 | nM | IC50 | Data for DCP probe BAY-1797 |
| ChEMBL | Fluorometric imaging plate reader (FLIPR)-based Ca2+ assay with HEK293 cells | B | 6.68 | pIC50 | 211 | nM | IC50 | Data for DCP probe BAY-1797 |
| ChEMBL | Antagonist activity at human P2X4 receptor tranfected in HEK293 cells assessed as inhibition of Bz-ATP-induced calcium influx incubated for 30 mins and measured every 2 secs for 120 secs by Fluo8-AM staining based FLIPR assay | B | 6.68 | pIC50 | 211 | nM | IC50 | J Med Chem (2019) 62: 11194-11217 [PMID:31746599] |
| ChEMBL | Fluorometric imaging plate reader (FLIPR)-based Ca2+ assay with 1321 N1 Astrocytoma cells | B | 6.97 | pIC50 | 108 | nM | IC50 | Data for DCP probe BAY-1797 |
| ChEMBL | Antagonist activity at human P2X4 receptor tranfected in human 1321N1 cells assessed as inhibition of Mg-ATP-induced calcium influx incubated for 30 mins and measured every 2 secs for 120 secs by Fluo8-AM staining based FLIPR assay | B | 6.97 | pIC50 | 108 | nM | IC50 | J Med Chem (2019) 62: 11194-11217 [PMID:31746599] |
| GtoPdb | - | - | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2019) 62: 11194-11217 [PMID:31746599] |
| P2X4/P2X purinoceptor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176849] [GtoPdb: 481] [UniProtKB: Q9JJX6] | ||||||||
| ChEMBL | Antagonist activity at mouse P2X4 receptor tranfected in human 1321N1 cells assessed as inhibition of Mg-ATP-induced calcium influx incubated for 30 mins and measured every 2 secs for 120 secs by Fluo8-AM staining based FLIPR assay | B | 6.95 | pIC50 | 112 | nM | IC50 | J Med Chem (2019) 62: 11194-11217 [PMID:31746599] |
| P2X4/P2X purinoceptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2818] [GtoPdb: 481] [UniProtKB: P51577] | ||||||||
| ChEMBL | Antagonist activity at rat P2X4 receptor tranfected in human 1321N1 cells assessed as inhibition of Mg-ATP-induced calcium influx incubated for 30 mins and measured every 2 secs for 120 secs by Fluo8-AM staining based FLIPR assay | B | 6.63 | pIC50 | 233 | nM | IC50 | J Med Chem (2019) 62: 11194-11217 [PMID:31746599] |
| P2X7/P2X purinoceptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572] | ||||||||
| ChEMBL | Antagonist activity at human P2X7 receptor | B | 4.97 | pIC50 | 10600 | nM | IC50 | J Med Chem (2019) 62: 11194-11217 [PMID:31746599] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of 5-HT2C | B | 5.19 | pKi | 6519.91 | nM | Ki | Data for DCP probe BAY-1797 |
| ChEMBL | GPCRScan assay: inhibition of 5-HT2C | B | 5.23 | pKi | 5888.44 | nM | Ki | Data for DCP probe BAY-1797 |
| σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of Sigma 2 | B | 5.36 | pKi | 4344.21 | nM | Ki | Data for DCP probe BAY-1797 |
| ChEMBL | GPCRScan assay: inhibition of Sigma 2 | B | 5.38 | pKi | 4168.69 | nM | Ki | Data for DCP probe BAY-1797 |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
