BMS-193884 [Ligand Id: 13016] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL24461 (BMS-193884) |
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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] | ||||||||
| GtoPdb | - | - | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2000) 43: 3111-7 [PMID:10956219] |
| ChEMBL | Compound was evaluated for its binding affinity towards human Endothelin A receptor | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2002) 45: 3829-3835 [PMID:12190306] |
| ChEMBL | Inhibitory concentration against Endothelin A receptor | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
| ChEMBL | Binding affinity to CHO cells stably expressing human Endothelin A receptor. | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 517-520 [PMID:11844662] |
| ChEMBL | Inhibitory activity against human endothelin A receptor expressed in CHO cells | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2003) 46: 125-137 [PMID:12502366] |
| ChEMBL | Inhibition of Human Endothelin A receptor expressed in CHO Cells. | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2000) 43: 3111-3117 [PMID:10956219] |
| ChEMBL | Binding affinity to ETA receptor | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2012) 55: 9363-9392 [PMID:22931505] |
| ETA receptor/Endothelin receptor ET-A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684] | ||||||||
| ChEMBL | Binding affinity towards Endothelin A receptor | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2004) 47: 1969-1986 [PMID:15055997] |
| ChEMBL | Displacement of [125I]-ET1 from ETA receptor in A10 rat thoracic aorta smooth muscle after 3 hrs by scintillation counting method | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813] |
| ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530] | ||||||||
| ChEMBL | Inhibitory concentration against endotheline ETB receptor | F | 4.73 | pKi | 18700 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
| ChEMBL | Binding affinity to CHO cells stably expressing human Endothelin B receptor. | B | 4.73 | pKi | 18700 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 517-520 [PMID:11844662] |
| ChEMBL | Inhibitory activity against human endothelin B receptor expressed in CHO cells | B | 4.73 | pKi | 18700 | nM | Ki | J Med Chem (2003) 46: 125-137 [PMID:12502366] |
| ChEMBL | Inhibition of Human Endothelin B receptor expressed in CHO Cells. | B | 4.73 | pKi | 18700 | nM | Ki | J Med Chem (2000) 43: 3111-3117 [PMID:10956219] |
| GtoPdb | - | - | 4.73 | pKi | 18700 | nM | Ki | J Med Chem (2000) 43: 3111-7 [PMID:10956219] |
| ETB receptor/Endothelin receptor ET-B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4631] [GtoPdb: 220] [UniProtKB: P21451] | ||||||||
| ChEMBL | Displacement of [125I]-ET1 from ETB receptor in rat cerebellum after 3 hrs by scintillation counting method | B | 5.72 | pKi | 1900 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813] |
| AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556] | ||||||||
| ChEMBL | Binding affinity to AT1 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2012) 55: 9363-9392 [PMID:22931505] |
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]
