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Assay Detail

CHEMBL643796

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

Binding
Displacement of [125 I]Sar1Ile8-AII from AT2 receptor of rat midbrain membrane
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Midbrain
Confidence 9 — Direct single protein target
Curated By Expert

Target

Type-2 angiotensin II receptor (CHEMBL257)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 8.85 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289472 1 10.22
CHEMBL34082 1 9.66
CHEMBL290768 1 9.62
CHEMBL290669 1 9.46
CHEMBL285433 1 9.34
CHEMBL108981 1 9.22
CHEMBL287250 1 9.15
CHEMBL35324 1 9.13
CHEMBL276853 1 9.00
CHEMBL35638 1 9.00
CHEMBL285432 1 8.85
CHEMBL284123 1 8.48
CHEMBL37919 1 7.48
CHEMBL24322 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289472 IC50 = 0.06 nM 10.22
CHEMBL34082 IC50 = 0.22 nM 9.66
CHEMBL290768 IC50 = 0.24 nM 9.62
CHEMBL290669 IC50 = 0.35 nM 9.46
CHEMBL285433 IC50 = 0.46 nM 9.34
CHEMBL108981 IC50 = 0.6 nM 9.22
CHEMBL287250 IC50 = 0.7 nM 9.15
CHEMBL35324 IC50 = 0.74 nM 9.13
CHEMBL276853 IC50 = 1.0 nM 9.00
CHEMBL35638 IC50 = 1.0 nM 9.00
CHEMBL285432 IC50 = 1.4 nM 8.85
CHEMBL284123 IC50 = 3.3 nM 8.48
CHEMBL37919 IC50 = 33.0 nM 7.48
CHEMBL24322 IC50 = 4500.0 nM 5.35