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Assay Detail

CHEMBL4839255

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Functional
Antagonist activity at human AT1 overexpressed in CHO-K1 cells in presence of 10 nM [Val5-angiotensin II measured after 90 mins by HTRF based IP-one assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of Irbesartan Derivatives as BLT2 Agonists by Virtual Screening.
Hernandez-Olmos V, Heering J, Bischoff-Kont I, Kaps A, Rajkumar R, Liu T, Fürst R, Steinhilber D, Proschak E.
ACS Med Chem Lett (2021) 12 : 1261 -1266
PubMed 34413955 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.57 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1513 IRBESARTAN 4.0 1 8.22
CHEMBL4872989 1 7.82
CHEMBL4856425 1 7.60
CHEMBL4877651 1 7.50
CHEMBL116170 1 6.81
CHEMBL439968 1 6.72
CHEMBL4859498 1 6.41
CHEMBL4868159 1 6.00
CHEMBL444060 1 5.11
CHEMBL115771 1 5.06
CHEMBL4854916 1 5.00
CHEMBL423325 1 -
CHEMBL4850970 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1513 IRBESARTAN IC50 = 6.0 nM 8.22
CHEMBL4872989 IC50 = 15.0 nM 7.82
CHEMBL4856425 IC50 = 25.0 nM 7.60
CHEMBL4877651 IC50 = 32.0 nM 7.50
CHEMBL116170 IC50 = 155.0 nM 6.81
CHEMBL439968 IC50 = 190.0 nM 6.72
CHEMBL4859498 IC50 = 390.0 nM 6.41
CHEMBL4868159 IC50 = 1010.0 nM 6.00
CHEMBL444060 IC50 = 7750.0 nM 5.11
CHEMBL115771 IC50 = 8650.0 nM 5.06
CHEMBL4854916 IC50 = 10000.0 nM 5.00
CHEMBL423325 IC50 > 10000.0 nM -
CHEMBL4850970 IC50 - -