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Assay Detail

CHEMBL4839253

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Functional
Agonist activity at human BLT2 overexpressed in CHO-K1 cells assessed as accumulation of inositol monophosphate measured after 90 mins by HTRF assay
22
Total Activities
22
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

Leukotriene B4 receptor 2 (CHEMBL3191)
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
EC50 22 5.55 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4872989 1 7.17
CHEMBL1513 IRBESARTAN 4.0 1 6.39
CHEMBL4856425 1 6.26
CHEMBL116170 1 6.07
CHEMBL439968 1 5.83
CHEMBL4859498 1 5.19
CHEMBL115771 1 5.18
CHEMBL4854916 1 5.12
CHEMBL4877651 1 5.09
CHEMBL1016 CANDESARTAN 3.0 1 4.82
CHEMBL1069 VALSARTAN 4.0 1 4.80
CHEMBL444060 1 4.62
CHEMBL240597 CHENODIOL 4.0 1 -
CHEMBL423325 1 -
CHEMBL267744 TICRYNAFEN 4.0 1 -
CHEMBL4850970 1 -
CHEMBL1765291 ZALTOPROFEN 2.0 1 -
CHEMBL152557 1 -
CHEMBL3707395 ELAFIBRANOR 4.0 1 -
CHEMBL2386081 SETIPIPRANT 3.0 1 -
CHEMBL57242 AZILSARTAN 3.0 1 -
CHEMBL4868159 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4872989 EC50 = 67.6 nM 7.17
CHEMBL1513 IRBESARTAN EC50 = 410.0 nM 6.39
CHEMBL4856425 EC50 = 550.0 nM 6.26
CHEMBL116170 EC50 = 860.0 nM 6.07
CHEMBL439968 EC50 = 1490.0 nM 5.83
CHEMBL4859498 EC50 = 6390.0 nM 5.19
CHEMBL115771 EC50 = 6580.0 nM 5.18
CHEMBL4854916 EC50 = 7500.0 nM 5.12
CHEMBL4877651 EC50 = 8140.0 nM 5.09
CHEMBL1016 CANDESARTAN EC50 = 15000.0 nM 4.82
CHEMBL1069 VALSARTAN EC50 = 16000.0 nM 4.80
CHEMBL444060 EC50 = 24200.0 nM 4.62
CHEMBL240597 CHENODIOL EC50 - -
CHEMBL423325 EC50 - -
CHEMBL267744 TICRYNAFEN EC50 - -
CHEMBL4850970 EC50 - -
CHEMBL1765291 ZALTOPROFEN EC50 - -
CHEMBL152557 EC50 - -
CHEMBL3707395 ELAFIBRANOR EC50 - -
CHEMBL2386081 SETIPIPRANT EC50 - -
CHEMBL57242 AZILSARTAN EC50 - -
CHEMBL4868159 EC50 - -