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Assay Detail

CHEMBL770464

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

Functional
Inhibition of angiotensin II-induced contractions in rabbit aorta in vitro.
21
Total Activities
21
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

Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
Wexler RR, Greenlee WJ, Irvin JD, Goldberg MR, Prendergast K, Smith RD, Timmermans PB.
J Med Chem (1996) 39 : 625 -656
PubMed 8576904 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 21 8.77 10.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL47177 1 10.90
CHEMBL416477 1 10.70
CHEMBL293511 1 10.30
CHEMBL418226 1 10.30
CHEMBL907 CARBOXYLIC ACID METABOLITE 1 10.09
CHEMBL41194 PRATOSARTAN 2.0 1 10.04
CHEMBL433895 1 9.20
CHEMBL48602 1 9.00
CHEMBL352257 1 8.82
CHEMBL71162 1 8.70
CHEMBL347610 1 8.65
CHEMBL191 LOSARTAN 4.0 1 8.48
CHEMBL158725 1 8.45
CHEMBL432162 TASOSARTAN 2.0 1 8.40
CHEMBL284536 1 8.30
CHEMBL315021 FORASARTAN 2.0 1 8.18
CHEMBL275875 CL-329167 1 8.01
CHEMBL262958 1 7.20
CHEMBL341716 1 7.10
CHEMBL158794 1 6.90
CHEMBL25686 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL47177 Kd = 0.01259 nM 10.90
CHEMBL416477 Kd = 0.01995 nM 10.70
CHEMBL293511 Kd = 0.05012 nM 10.30
CHEMBL418226 Kd = 0.05012 nM 10.30
CHEMBL907 CARBOXYLIC ACID METABOLITE Kd = 0.08128 nM 10.09
CHEMBL41194 PRATOSARTAN Kd = 0.0912 nM 10.04
CHEMBL433895 Kd = 0.631 nM 9.20
CHEMBL48602 Kd = 1.0 nM 9.00
CHEMBL352257 Kd = 1.514 nM 8.82
CHEMBL71162 Kd = 1.995 nM 8.70
CHEMBL347610 Kd = 2.239 nM 8.65
CHEMBL191 LOSARTAN Kd = 3.311 nM 8.48
CHEMBL158725 Kd = 3.548 nM 8.45
CHEMBL432162 TASOSARTAN Kd = 3.981 nM 8.40
CHEMBL284536 Kd = 5.012 nM 8.30
CHEMBL315021 FORASARTAN Kd = 6.607 nM 8.18
CHEMBL275875 CL-329167 Kd = 9.772 nM 8.01
CHEMBL262958 Kd = 63.1 nM 7.20
CHEMBL341716 Kd = 79.43 nM 7.10
CHEMBL158794 Kd = 125.89 nM 6.90
CHEMBL25686 Kd = 288.4 nM 6.54