Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL907 (E-3174) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
Angiotensin II type 1a (AT-1a) receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3374] [UniProtKB: P25104] | ||||||||
ChEMBL | In vitro for inhibition of [125I]-angiotensin II (0.1 nM) binding to angiotensin II receptor type 1 in membrane fractions of bovine adrenal cortex | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (1996) 39: 323-338 [PMID:8568823] |
ChEMBL | Inhibition of [125l]-All binding to bovine adrenal cortex | B | 7.66 | pIC50 | 22 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 177-182 |
Angiotensin II type 1a (AT-1a) receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3948] [UniProtKB: P34976] | ||||||||
ChEMBL | Antagonist activity at angiotensin AT1 receptor in rabbit aorta assessed as reduction of angiotensin 2-induced contractile response | F | 10.09 | pKd | 0.08 | nM | Kd | Bioorg Med Chem (2010) 18: 8418-8456 [PMID:21071232] |
ChEMBL | In vitro antagonistic activity for AT1 receptor by displacing 125I[Sar, ILe8]AII radioligand in rabbit aorta membrane using 0.2% bovine serum albumin (BSA) | F | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (1993) 36: 2558-2568 [PMID:8355255] |
ChEMBL | In vitro binding affinity for angiotensin II AT1 receptor in rabbit aorta | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1994) 37: 4068-4072 [PMID:7990105] |
ChEMBL | Displacement of [125I]-Sar1-Ile8-A II at the rabbit aorta angiotensin II receptor, type 1 | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1993) 36: 591-609 [PMID:8496939] |
ChEMBL | In vitro antagonistic activity for angiotensin II receptor, type 1 by displacing 125I[Sar, ILe8 ]AII radioligand in rabbit aorta membrane without using bovine serum albumin (BSA) | F | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1993) 36: 2558-2568 [PMID:8355255] |
ChEMBL | Evaluation of Angiotensin II antagonistic activity by displacement of [125I]-Sar Ile-AII at the rabbit aorta Angiotensin II receptor, type 1 | F | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (1993) 36: 3595-3605 [PMID:8246227] |
ChEMBL | In vitro inhibitory activity against angiotensin II rabbit aorta AT1 receptor using radioligand [125I]-Sar Ile-AII | B | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (1994) 37: 2808-2824 [PMID:8064808] |
AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL257] [GtoPdb: 35] [UniProtKB: P35351] | ||||||||
ChEMBL | In vitro inhibitory activity against angiotensin II rat midbrain AT2 receptor using radioligand [125I]-Sar Ile-AII | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (1994) 37: 2808-2824 [PMID:8064808] |
ChEMBL | In vitro binding affinity for angiotensin II AT2 receptor in rat midbrain | B | 4.3 | pIC50 | 50000 | nM | IC50 | J Med Chem (1994) 37: 4068-4072 [PMID:7990105] |
AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556] | ||||||||
ChEMBL | Inhibition of ATR1 (unknown origin) | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2019) 62: 8915-8930 [PMID:31083946] |
GtoPdb | - | - | 9.49 | pIC50 | 0.32 | nM | IC50 |
Br J Pharmacol (1999) 126: 1057-65 [PMID:10193788]; Pharmacol Rev (1993) 45: 205-51 [PMID:8372104] |
AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556] | ||||||||
GtoPdb | - | - | 9.49 | pIC50 | 0.32 | nM | IC50 |
Br J Pharmacol (1999) 126: 1057-65 [PMID:10193788]; Pharmacol Rev (1993) 45: 205-51 [PMID:8372104] |
AT1 receptor/Type-1B angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL263] [GtoPdb: 34] [UniProtKB: P29089] | ||||||||
ChEMBL | In vitro antagonistic activity by displacement of [125I]-Sar1-Ile8-A II at the rabbit aorta Angiotensin II receptor, type 1 | F | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (1993) 36: 591-609 [PMID:8496939] |
ChEMBL | Concentration required to inhibit binding of radioligand [125I]AII to Angiotensin II receptor, type 1 in rat adrenal glomerulosa tissue | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (1992) 35: 2658-2667 [PMID:1635064] |
ChEMBL | Binding affinity against AT1 receptor in the presence of 0.01% BSA | B | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (1994) 37: 1632-1645 [PMID:8201597] |
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]