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Assay Detail

CHEMBL651545

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

Binding
Tested in vitro for inhibition of [125I]AII to rat uterine membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Angiotensin II receptor (CHEMBL2094112)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

1H-1,2,4-triazole angiotensin II receptor antagonists: N-phenylpyridinylmethyl and N-pyridinylphenylmethyl analogs of SC-50560
Reitz DB, Penick MA, Reinhard EJ, Cheng BK, Olins GM, Corpus VM, Palomo MA, McGraw DE, McMahon EG
Bioorg Med Chem Lett (1994) 4 : 99 -104
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.43 8.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85595 1 8.25
CHEMBL315022 1 8.17
CHEMBL315021 FORASARTAN 2.0 1 8.16
CHEMBL191 LOSARTAN 4.0 1 7.44
CHEMBL86344 1 7.01
CHEMBL88067 1 6.96
CHEMBL87411 1 6.82
CHEMBL87655 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85595 IC50 = 5.6 nM 8.25
CHEMBL315022 IC50 = 6.8 nM 8.17
CHEMBL315021 FORASARTAN IC50 = 6.9 nM 8.16
CHEMBL191 LOSARTAN IC50 = 36.0 nM 7.44
CHEMBL86344 IC50 = 98.0 nM 7.01
CHEMBL88067 IC50 = 110.0 nM 6.96
CHEMBL87411 IC50 = 150.0 nM 6.82
CHEMBL87655 IC50 = 250.0 nM 6.60