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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
