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 | Eurofins cellular functional assay - Antagonist (EDNRA) | F | 5.44 | pIC50 | 3600 | 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 | Affinity Biochemical interaction (Inhibition of 125I labeled ET-3 binding) EUB0000350a EDNRB | B | 8.35 | pIC50 | 4.5 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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 | Affinity On-target Cellular interaction (EDNRB-dependent phosphatidylinositol hydrolysis assay (CHO cells transfected with human EDNRBA)) EUB0000350a EDNRB | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Affinity Phenotypic Cellular interaction (Agonist activity for hGPR54 (C-terminal ethyl amide)) EUB0000350a EDNRB | B | 5 | pEC50 | >10000 | nM | EC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
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]
