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Assay Detail

CHEMBL3872473

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

Binding
Displacement of 125I-Ang2 from AT1 receptor in SPF Sprague-Dawley rat vascular smooth muscle cell membranes after 150 mins by gamma counting method
16
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, synthesis and evaluation of novel potent angiotensin II receptor 1 antagonists.
Bao X, Zhu W, Yuan W, Zhu X, Yan Y, Tang H, Chen Z.
Eur J Med Chem (2016) 123 : 115 -127
PubMed 27474928 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.54 9.04
IC50 8 8.40 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3936495 2 9.04
CHEMBL1513 IRBESARTAN 4.0 2 8.98
CHEMBL3893900 2 8.66
CHEMBL3974791 2 8.47
CHEMBL3945382 2 8.33
CHEMBL3962847 2 8.33
CHEMBL3966294 2 8.29
CHEMBL3954111 2 8.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3936495 Ki = 0.91 nM 9.04
CHEMBL1513 IRBESARTAN Ki = 1.05 nM 8.98
CHEMBL3936495 IC50 = 1.26 nM 8.90
CHEMBL1513 IRBESARTAN IC50 = 1.46 nM 8.84
CHEMBL3893900 Ki = 2.21 nM 8.66
CHEMBL3893900 IC50 = 3.05 nM 8.52
CHEMBL3974791 Ki = 3.42 nM 8.47
CHEMBL3945382 Ki = 4.67 nM 8.33
CHEMBL3962847 Ki = 4.67 nM 8.33
CHEMBL3966294 Ki = 5.07 nM 8.29
CHEMBL3974791 IC50 = 5.33 nM 8.27
CHEMBL3954111 Ki = 5.61 nM 8.25
CHEMBL3945382 IC50 = 6.15 nM 8.21
CHEMBL3962847 IC50 = 6.15 nM 8.21
CHEMBL3966294 IC50 = 7.04 nM 8.15
CHEMBL3954111 IC50 = 7.75 nM 8.11