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Assay Detail

CHEMBL647799

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

Binding
Displacement of [125I]- Ang II from angiotensin II AT1 receptor in rat adrenal cortical microsomes
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Balanced angiotensin II receptor antagonists. I. The effects of biphenyl ortho-substitution on AT1/AT2 affinities
Quan ML, Olson RE, Carini DJ, Ellis CD, Hillyer GL, Lalka GK, Liu J, VanAtten MK, Chiu AT, Wong PC, Wexler RR, Timmermans PB
Bioorg Med Chem Lett (1994) 4 : 2011 -2016
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.56 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL63998 1 9.52
CHEMBL64411 1 9.22
CHEMBL431162 1 9.15
CHEMBL60942 1 9.00
CHEMBL294512 1 9.00
CHEMBL59331 1 8.70
CHEMBL59611 1 8.70
CHEMBL291582 1 8.70
CHEMBL60992 1 8.70
CHEMBL417393 1 8.70
CHEMBL294578 1 8.70
CHEMBL59957 1 8.62
CHEMBL291803 1 8.52
CHEMBL443269 1 8.52
CHEMBL304022 1 8.52
CHEMBL60661 1 8.52
CHEMBL61168 1 8.52
CHEMBL431137 1 8.22
CHEMBL59728 1 8.15
CHEMBL439936 1 8.15
CHEMBL61754 1 8.00
CHEMBL59974 1 7.70
CHEMBL61976 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL63998 IC50 = 0.3 nM 9.52
CHEMBL64411 IC50 = 0.6 nM 9.22
CHEMBL431162 IC50 = 0.7 nM 9.15
CHEMBL60942 IC50 = 1.0 nM 9.00
CHEMBL294512 IC50 = 1.0 nM 9.00
CHEMBL59331 IC50 = 2.0 nM 8.70
CHEMBL59611 IC50 = 2.0 nM 8.70
CHEMBL291582 IC50 = 2.0 nM 8.70
CHEMBL60992 IC50 = 2.0 nM 8.70
CHEMBL417393 IC50 = 2.0 nM 8.70
CHEMBL294578 IC50 = 2.0 nM 8.70
CHEMBL59957 IC50 = 2.4 nM 8.62
CHEMBL291803 IC50 = 3.0 nM 8.52
CHEMBL443269 IC50 = 3.0 nM 8.52
CHEMBL304022 IC50 = 3.0 nM 8.52
CHEMBL60661 IC50 = 3.0 nM 8.52
CHEMBL61168 IC50 = 3.0 nM 8.52
CHEMBL431137 IC50 = 6.0 nM 8.22
CHEMBL59728 IC50 = 7.0 nM 8.15
CHEMBL439936 IC50 = 7.0 nM 8.15
CHEMBL61754 IC50 = 10.0 nM 8.00
CHEMBL59974 IC50 = 20.0 nM 7.70
CHEMBL61976 IC50 = 40.0 nM 7.40