Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1669998

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

Functional
Antagonist activity at angiotensin AT1 receptor
15
Total Activities
15
Compounds Tested
4
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
Kd 11 8.96 10.90
IC50 2 9.07 9.40
Kb 1 - -
pD2 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL47177 1 10.90
CHEMBL275875 CL-329167 1 10.90
CHEMBL34866 1 9.40
CHEMBL9599 SC-55634 1 9.30
CHEMBL45927 1 9.30
CHEMBL24224 1 8.74
CHEMBL85595 1 8.70
CHEMBL9642 SC-52892 1 8.68
CHEMBL9714 SC-51895 1 8.65
CHEMBL12909 1 8.50
CHEMBL191 LOSARTAN 4.0 1 8.48
CHEMBL315021 FORASARTAN 2.0 1 8.20
CHEMBL158794 1 6.90
CHEMBL358335 1 -
CHEMBL1016 CANDESARTAN 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL47177 Kd = 0.01259 nM 10.90
CHEMBL275875 CL-329167 Kd = 0.01259 nM 10.90
CHEMBL34866 IC50 = 0.4 nM 9.40
CHEMBL9599 SC-55634 Kd = 0.5012 nM 9.30
CHEMBL45927 Kd = 0.5012 nM 9.30
CHEMBL24224 IC50 = 1.8 nM 8.74
CHEMBL85595 Kd = 1.995 nM 8.70
CHEMBL9642 SC-52892 Kd = 2.089 nM 8.68
CHEMBL9714 SC-51895 Kd = 2.239 nM 8.65
CHEMBL12909 Kd = 3.162 nM 8.50
CHEMBL191 LOSARTAN Kd = 3.311 nM 8.48
CHEMBL315021 FORASARTAN Kd = 6.31 nM 8.20
CHEMBL158794 Kd = 125.89 nM 6.90
CHEMBL358335 Kb = 0.45 nM -
CHEMBL1016 CANDESARTAN pD2 = 9.97 -