PD-156707 [Ligand Id: 999] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL25438 (PD-156707) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ETA receptor/Endothelin receptor ET-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101] | ||||||||
| ChEMBL | pA2 value towards endothelin receptor A was determined as functional ETA antagonism | F | 7.6 | pKd | 25.12 | nM | Kd | Bioorg Med Chem Lett (1998) 8: 17-22 [PMID:9871621] |
| GtoPdb | - | - | 9.8 | pKd | 0.15 | nM | Kd | J Pharmacol Exp Ther (1997) 280: 1102-8 [PMID:9023329] |
| ChEMBL | Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO) | B | 9.77 | pKi | 0.17 | nM | Ki | J Med Chem (1998) 41: 3261-3275 [PMID:9703472] |
| ChEMBL | Antagonistic activity against human Endothelin A receptor expressed in LtK | F | 9.51 | pIC50 | 0.31 | nM | IC50 | J Med Chem (1995) 38: 1259-1263 [PMID:7731010] |
| GtoPdb | - | - | 9.2 | pA2 | - | - | - |
Stroke (1999) 30: 638-43 [PMID:10066864]; J Pharmacol Exp Ther (1997) 280: 1102-8 [PMID:9023329] |
| ETA receptor/Endothelin receptor ET-A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684] | ||||||||
| ChEMBL | In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1771-1776 [PMID:9873432] |
| ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530] | ||||||||
| ChEMBL | Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO) | B | 6.86 | pKi | 139 | nM | Ki | J Med Chem (1998) 41: 3261-3275 [PMID:9703472] |
| ChEMBL | Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed). | F | 6.38 | pIC50 | 417 | nM | IC50 | J Med Chem (1995) 38: 1259-1263 [PMID:7731010] |
| Endothelin receptor ET-B in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3949] [UniProtKB: P35463] | ||||||||
| ChEMBL | In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor | B | 6.47 | pIC50 | 340 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1771-1776 [PMID:9873432] |
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]
