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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 |
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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 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]