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Assay Detail

CHEMBL650273

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

Binding
Displacement of [125 I]Sar1Ile8-AII from type 1 Angiotensin II receptor of rabbit aorta membrane
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Aorta
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Type-1 angiotensin II receptor (CHEMBL3948)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

L-161,638: A potent AT2selective quinazolinone angiotensin II binding inhibitor
Glinka TW, de Laszlo SE, Tran J, Chang RS, Chen T, Lotti VJ, Greenlee WJ
Bioorg Med Chem Lett (1994) 4 : 1479 -1484
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.28 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24322 1 10.00
CHEMBL287250 1 8.77
CHEMBL108981 1 8.31
CHEMBL37919 1 8.29
CHEMBL290768 1 7.38
CHEMBL34082 1 7.14
CHEMBL276853 1 7.10
CHEMBL284123 1 6.80
CHEMBL35638 1 6.77
CHEMBL289472 1 6.70
CHEMBL285433 1 6.39
CHEMBL285432 1 6.23
CHEMBL35324 1 6.09
CHEMBL290669 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24322 IC50 = 0.1 nM 10.00
CHEMBL287250 IC50 = 1.7 nM 8.77
CHEMBL108981 IC50 = 4.9 nM 8.31
CHEMBL37919 IC50 = 5.1 nM 8.29
CHEMBL290768 IC50 = 42.0 nM 7.38
CHEMBL34082 IC50 = 72.0 nM 7.14
CHEMBL276853 IC50 = 79.0 nM 7.10
CHEMBL284123 IC50 = 160.0 nM 6.80
CHEMBL35638 IC50 = 170.0 nM 6.77
CHEMBL289472 IC50 = 200.0 nM 6.70
CHEMBL285433 IC50 = 410.0 nM 6.39
CHEMBL285432 IC50 = 590.0 nM 6.23
CHEMBL35324 IC50 = 820.0 nM 6.09
CHEMBL290669 IC50 = 1200.0 nM 5.92