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Assay Detail

CHEMBL652261

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Evaluated in vitro for antagonism of AII induced contraction of isolated rabbit aorta
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Aorta
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Angiotensin II receptor (CHEMBL2094256)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Cycloheptimidazole based angiotensin II receptor antagonists. 4,5,6,7-tetrahydro-8-carboxymethylidene cycloheptimidazoles
Ueyama N, Yanagisawa T, Hiromi B, Keiko K, Hiromi H, Motoharu S, Tsuyoshi T
Bioorg Med Chem Lett (1994) 4 : 1637 -1642
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 15 8.66 10.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41194 PRATOSARTAN 2.0 1 10.01
CHEMBL44295 1 9.80
CHEMBL289391 1 9.80
CHEMBL43540 1 9.66
CHEMBL43530 1 9.64
CHEMBL290848 1 9.52
CHEMBL443000 1 9.30
CHEMBL288832 1 9.03
CHEMBL297637 1 8.90
CHEMBL298080 1 8.80
CHEMBL42984 1 8.02
CHEMBL43861 1 7.85
CHEMBL43814 1 7.00
CHEMBL46628 1 6.31
CHEMBL42070 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41194 PRATOSARTAN Kd = 0.09772 nM 10.01
CHEMBL44295 Kd = 0.1585 nM 9.80
CHEMBL289391 Kd = 0.1585 nM 9.80
CHEMBL43540 Kd = 0.2188 nM 9.66
CHEMBL43530 Kd = 0.2291 nM 9.64
CHEMBL290848 Kd = 0.302 nM 9.52
CHEMBL443000 Kd = 0.5012 nM 9.30
CHEMBL288832 Kd = 0.9333 nM 9.03
CHEMBL297637 Kd = 1.259 nM 8.90
CHEMBL298080 Kd = 1.585 nM 8.80
CHEMBL42984 Kd = 9.55 nM 8.02
CHEMBL43861 Kd = 14.13 nM 7.85
CHEMBL43814 Kd = 100.0 nM 7.00
CHEMBL46628 Kd = 489.78 nM 6.31
CHEMBL42070 Kd = 588.84 nM 6.23