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Assay Detail

CHEMBL643791

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

Binding
Inhibitory activity against angiotensin II type 2 (AT2) receptor in rabbit uterine membranes.
21
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Type-2 angiotensin II receptor (CHEMBL4607)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tetrahydroisoquinoline derivatives with AT2-specific angiotensin II reception binding inhibitory activity
Klutchko S, Hamby JM, Hodges JC
Bioorg Med Chem Lett (1994) 4 : 57 -62
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.65 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157510 1 9.24
CHEMBL155836 2 9.08
CHEMBL290829 1 9.05
CHEMBL154057 1 8.96
CHEMBL156100 1 8.72
CHEMBL156129 1 8.32
CHEMBL348363 1 8.24
CHEMBL157946 1 8.16
CHEMBL155728 1 8.03
CHEMBL156165 1 7.46
CHEMBL156587 1 7.40
CHEMBL155987 1 7.23
CHEMBL155938 1 7.16
CHEMBL423236 1 6.82
CHEMBL155847 1 6.77
CHEMBL128416 1 6.70
CHEMBL160930 1 6.43
CHEMBL350875 1 6.14
CHEMBL158557 1 6.12
CHEMBL350220 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157510 IC50 = 0.58 nM 9.24
CHEMBL155836 IC50 = 0.84 nM 9.08
CHEMBL290829 IC50 = 0.89 nM 9.05
CHEMBL154057 IC50 = 1.1 nM 8.96
CHEMBL156100 IC50 = 1.9 nM 8.72
CHEMBL155836 IC50 = 2.4 nM 8.62
CHEMBL156129 IC50 = 4.8 nM 8.32
CHEMBL348363 IC50 = 5.8 nM 8.24
CHEMBL157946 IC50 = 6.9 nM 8.16
CHEMBL155728 IC50 = 9.4 nM 8.03
CHEMBL156165 IC50 = 35.0 nM 7.46
CHEMBL156587 IC50 = 40.0 nM 7.40
CHEMBL155987 IC50 = 59.0 nM 7.23
CHEMBL155938 IC50 = 70.0 nM 7.16
CHEMBL423236 IC50 = 150.0 nM 6.82
CHEMBL155847 IC50 = 170.0 nM 6.77
CHEMBL128416 IC50 = 200.0 nM 6.70
CHEMBL160930 IC50 = 370.0 nM 6.43
CHEMBL350875 IC50 = 730.0 nM 6.14
CHEMBL158557 IC50 = 750.0 nM 6.12
CHEMBL350220 IC50 = 1100.0 nM 5.96