SB209670 [Ligand Id: 3528] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL8823 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ETA receptor/Endothelin-1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101] | ||||||||
| ChEMBL | Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cells | B | 9.37 | pKi | 0.43 | nM | Ki | J Med Chem (1996) 39: 1039-1048 [PMID:8676339] |
| ChEMBL | Inhibition of [125I]ET1 binding to cloned human ET-A receptor | B | 9.37 | pKi | 0.43 | nM | Ki | J Med Chem (1994) 37: 1553-1557 [PMID:8201588] |
| ChEMBL | Ability to displace endothelin ([125I]ET1) from human Endothelin A receptor | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (1997) 40: 3217-3227 [PMID:9379441] |
| ChEMBL | Displacement of [125I]endhothelin-1 from human ETA receptor stably expressed in CHO cells Membrane at 30 degC incubated for 60 mins by radioligand competition binding assay | B | 9.7 | pKi | 0.2 | nM | Ki | Eur J Pharmacol (1999) 366: 189-201 [PMID:10082200] |
| ETA receptor in Rat [GtoPdb: 219] [UniProtKB: P26684] | ||||||||
| ETB receptor/Endothelin receptor type B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530] | ||||||||
| ChEMBL | Ability to displace endothelin ([125I]ET1) from human Endothelin B receptor | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (1997) 40: 3217-3227 [PMID:9379441] |
| ChEMBL | Displacement of [125I]endhothelin-1 from human ETB receptor stably expressed in CHO cells Membrane at 30 degC incubated for 60 mins by radioligand competition binding assay | B | 7.74 | pKi | 18 | nM | Ki | Eur J Pharmacol (1999) 366: 189-201 [PMID:10082200] |
| ChEMBL | Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cells | B | 7.83 | pKi | 14.7 | nM | Ki | J Med Chem (1996) 39: 1039-1048 [PMID:8676339] |
| ChEMBL | Inhibition of [125I]ET1 binding to cloned human ET-B receptor | B | 7.83 | pKi | 14.7 | nM | Ki | J Med Chem (1994) 37: 1553-1557 [PMID:8201588] |
| ETB receptor in Rat [GtoPdb: 220] [UniProtKB: P21451] | ||||||||
ChEMBL data shown on this page come from version 36:
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]
