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Assay Detail

CHEMBL647802

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

Binding
In vitro binding affinity for rat liver angiotensin II receptor type 1, determined by displacement of the specially bound [3H]AII radioligand
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Angiotensin II receptor (AT-1) type-1 (CHEMBL2094250)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis and structure-activity relationship of a new series of potent AT1 selective angiotensin II receptor antagonists: 5-(biphenyl-4-ylmethyl)pyrazoles.
Almansa C, Gómez LA, Cavalcanti FL, de Arriba AF, García-Rafanell J, Forn J.
J Med Chem (1997) 40 : 547 -558
PubMed 9046346 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 7.59 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL153268 1 8.66
CHEMBL907 CARBOXYLIC ACID METABOLITE 1 8.57
CHEMBL152106 1 8.52
CHEMBL153385 1 8.43
CHEMBL345979 1 8.36
CHEMBL357951 1 8.34
CHEMBL153013 1 8.17
CHEMBL356877 1 8.14
CHEMBL436617 1 8.13
CHEMBL152145 1 8.06
CHEMBL154931 1 8.05
CHEMBL443559 1 8.04
CHEMBL153045 1 8.03
CHEMBL153384 1 8.00
CHEMBL422149 1 8.00
CHEMBL358625 1 7.92
CHEMBL434888 1 7.89
CHEMBL153382 1 7.75
CHEMBL153457 1 7.72
CHEMBL153581 1 7.52
CHEMBL151856 1 7.26
CHEMBL191 LOSARTAN 4.0 1 7.23
CHEMBL433543 1 7.19
CHEMBL358236 1 7.16
CHEMBL435640 1 7.13
CHEMBL151346 1 7.13
CHEMBL358445 1 7.11
CHEMBL358396 1 7.03
CHEMBL153453 1 6.96
CHEMBL419963 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL153268 IC50 = 2.2 nM 8.66
CHEMBL907 CARBOXYLIC ACID METABOLITE IC50 = 2.7 nM 8.57
CHEMBL152106 IC50 = 3.0 nM 8.52
CHEMBL153385 IC50 = 3.7 nM 8.43
CHEMBL345979 IC50 = 4.4 nM 8.36
CHEMBL357951 IC50 = 4.6 nM 8.34
CHEMBL153013 IC50 = 6.7 nM 8.17
CHEMBL356877 IC50 = 7.3 nM 8.14
CHEMBL436617 IC50 = 7.4 nM 8.13
CHEMBL152145 IC50 = 8.7 nM 8.06
CHEMBL154931 IC50 = 9.0 nM 8.05
CHEMBL443559 IC50 = 9.1 nM 8.04
CHEMBL153045 IC50 = 9.3 nM 8.03
CHEMBL153384 IC50 = 10.0 nM 8.00
CHEMBL422149 IC50 = 9.9 nM 8.00
CHEMBL358625 IC50 = 12.0 nM 7.92
CHEMBL434888 IC50 = 13.0 nM 7.89
CHEMBL153382 IC50 = 18.0 nM 7.75
CHEMBL153457 IC50 = 19.0 nM 7.72
CHEMBL153581 IC50 = 30.0 nM 7.52
CHEMBL151856 IC50 = 55.0 nM 7.26
CHEMBL191 LOSARTAN IC50 = 59.0 nM 7.23
CHEMBL433543 IC50 = 65.0 nM 7.19
CHEMBL358236 IC50 = 70.0 nM 7.16
CHEMBL435640 IC50 = 74.0 nM 7.13
CHEMBL151346 IC50 = 74.0 nM 7.13
CHEMBL358445 IC50 = 78.0 nM 7.11
CHEMBL358396 IC50 = 94.0 nM 7.03
CHEMBL153453 IC50 = 110.0 nM 6.96
CHEMBL419963 IC50 = 120.0 nM 6.92
CHEMBL150608 IC50 = 130.0 nM 6.89
CHEMBL348705 IC50 = 290.0 nM 6.54
CHEMBL440358 IC50 = 350.0 nM 6.46
CHEMBL153340 IC50 = 490.0 nM 6.31
CHEMBL356846 IC50 = 770.0 nM 6.11