A192621 [Ligand Id: 1009] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL332794 (A-192621) |
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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 | 125I-labelled ET-1 saturation binding studies with EDNRA | B | 5.25 | pKi | 5600 | nM | Ki | Data for DCP probe A-192621 |
| ChEMBL | Binding affinity towards human Endothelin A receptor (hET -A) | B | 5 | pIC50 | 9900 | nM | IC50 | J Med Chem (1999) 42: 3668-3678 [PMID:10479298] |
| ChEMBL | Binding affinity towards human Endothelin A receptor (hET -A) | B | 5.09 | pIC50 | 8200 | nM | IC50 | J Med Chem (1999) 42: 3668-3678 [PMID:10479298] |
| ChEMBL | Inhibition of 125I labeled ET-1 binding to EDNRA | B | 5.37 | pIC50 | 4280 | nM | IC50 | Data for DCP probe A-192621 |
| ChEMBL | EDNRA- dependent phosphatidylinositol hydrolysis assay | F | 6 | pIC50 | >1000 | nM | IC50 | Data for DCP probe A-192621 |
| ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530] | ||||||||
| GtoPdb | - | - | 8.1 | pKd | 7.94 | nM | Kd | J Med Chem (1999) 42: 3668-78 [PMID:10479298] |
| ChEMBL | 125I-labelled ET-1 saturation binding studies with EDNRB | B | 8.06 | pKi | 8.8 | nM | Ki | Data for DCP probe A-192621 |
| ChEMBL | Binding affinity towards human Endothelin B receptor (hET -B) | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (1999) 42: 3668-3678 [PMID:10479298] |
| ChEMBL | Eurofins cellular functional assay - Antagonist (EDNRB) | F | 8.19 | pIC50 | 6.5 | nM | IC50 | Data for DCP probe A-192621 |
| ChEMBL | Binding affinity towards human Endothelin B receptor (hET -B) | B | 8.19 | pIC50 | 6.4 | nM | IC50 | J Med Chem (1999) 42: 3668-3678 [PMID:10479298] |
| ChEMBL | Inhibition of 125I labeled ET-3 binding to EDNRB | B | 8.35 | pIC50 | 4.5 | nM | IC50 | Data for DCP probe A-192621 |
| ChEMBL | EDNRB- dependent phosphatidylinositol hydrolysis assay | F | 9.1 | pIC50 | 0.8 | nM | IC50 | Data for DCP probe A-192621 |
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]
