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Assay Detail

CHEMBL1670336

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Binding
Binding affinity to angiotensin AT1 receptor
18
Total Activities
18
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Type-1 angiotensin II receptor (CHEMBL227)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
Naik P, Murumkar P, Giridhar R, Yadav MR.
Bioorg Med Chem (2010) 18 : 8418 -8456
PubMed 21071232 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.01 8.85
Ki 4 8.23 9.00
pKb 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL358335 1 9.00
CHEMBL157577 1 8.85
CHEMBL279629 L-159913 1 8.77
CHEMBL1668007 1 8.33
CHEMBL9599 SC-55634 1 8.31
CHEMBL85595 1 8.25
CHEMBL275875 CL-329167 1 8.22
CHEMBL9642 SC-52892 1 8.19
CHEMBL315021 FORASARTAN 2.0 1 8.16
CHEMBL9714 SC-51895 1 7.92
CHEMBL12909 1 7.80
CHEMBL267056 1 7.77
CHEMBL1513 IRBESARTAN 4.0 1 7.68
CHEMBL7396 1 7.66
CHEMBL312104 RIPISARTAN 2.0 1 7.62
CHEMBL1668003 1 7.54
CHEMBL1016 CANDESARTAN 3.0 1 6.96
CHEMBL1668123 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL358335 Ki = 1.0 nM 9.00
CHEMBL157577 IC50 = 1.4 nM 8.85
CHEMBL279629 L-159913 Ki = 1.7 nM 8.77
CHEMBL1668007 IC50 = 4.7 nM 8.33
CHEMBL9599 SC-55634 IC50 = 4.9 nM 8.31
CHEMBL85595 IC50 = 5.6 nM 8.25
CHEMBL275875 CL-329167 IC50 = 6.0 nM 8.22
CHEMBL9642 SC-52892 IC50 = 6.5 nM 8.19
CHEMBL315021 FORASARTAN IC50 = 6.9 nM 8.16
CHEMBL9714 SC-51895 IC50 = 12.0 nM 7.92
CHEMBL12909 IC50 = 16.0 nM 7.80
CHEMBL267056 IC50 = 17.0 nM 7.77
CHEMBL1513 IRBESARTAN IC50 = 20.8 nM 7.68
CHEMBL7396 IC50 = 22.0 nM 7.66
CHEMBL312104 RIPISARTAN Ki = 24.0 nM 7.62
CHEMBL1668003 Ki = 29.0 nM 7.54
CHEMBL1016 CANDESARTAN IC50 = 110.0 nM 6.96
CHEMBL1668123 pKb = 10.6 -