A192621 [Ligand Id: 1009] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL332794 |
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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 | 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 to human ETA receptor transfected in CHO cell membrane assessed as inhibition constant incubated for 3 hrs by 125I-labelled ET-1 saturation binding assay | B | 5.25 | pKi | 5600 | nM | Ki | Clin Sci (Lond) (2002) 103 Suppl 48: 107-111 [PMID:12193066] |
| 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 | Antagonist activity at human ETA receptor transfected in CHO cell membrane assessed as inhibition of 125I-labelled ET-1 binding to receptor incubated for 3 hrs by competition binding assay | F | 5.37 | pIC50 | 4280 | nM | IC50 | Clin Sci (Lond) (2002) 103 Suppl 48: 107-111 [PMID:12193066] |
| 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 |
| ETA receptor/Endothelin-1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684] | ||||||||
| ChEMBL | Antagonist activity at ETA receptor in rat MMQ cells assessed as inhibition of phosphatidylinositol hydrolysis by myo-[3H]inositol radioactivity based assay | F | 6.15 | pIC50 | >=700 | nM | IC50 | Clin Sci (Lond) (2002) 103 Suppl 48: 107-111 [PMID:12193066] |
| ETB receptor/Endothelin receptor type 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 to human ETB receptor transfected in CHO cell membrane assessed as inhibition constant incubated for 3 hrs by 125I-labelled ET-1 saturation binding assay | B | 8.06 | pKi | 8.8 | nM | Ki | Clin Sci (Lond) (2002) 103 Suppl 48: 107-111 [PMID:12193066] |
| 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 | Antagonist activity at human ETB receptor transfected in CHO cell membrane assessed as inhibition of 125I-labelled ET-3 binding to receptor incubated for 3 hrs by competition binding assay | F | 8.34 | pIC50 | 4.54 | nM | IC50 | Clin Sci (Lond) (2002) 103 Suppl 48: 107-111 [PMID:12193066] |
| 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 | 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 | EDNRB- dependent phosphatidylinositol hydrolysis assay | F | 9.1 | pIC50 | 0.8 | nM | IC50 | Data for DCP probe A-192621 |
| ChEMBL | Antagonist activity at human ETB receptor transfected in CHO cell membrane assessed as inhibition of phosphatidylinositol hydrolysis by myo-[3H]inositol radioactivity based assay | F | 9.23 | pIC50 | 0.59 | nM | IC50 | Clin Sci (Lond) (2002) 103 Suppl 48: 107-111 [PMID:12193066] |
| 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 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]
