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Assay Detail

CHEMBL1107473

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

Functional
Antagonist activity at FLAG-tagged human BLT1 receptor expressed in HEK293 cells assessed as inhibition of LTB4-stimulated calcium mobilization preincubated for 10 mins before LTB4 challenge
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Leukotriene B4 receptor 1 (CHEMBL3911)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel and potent leukotriene B4 receptor antagonists. Part 1.
Goodnow RA, Hicks A, Sidduri A, Kowalczyk A, Dominique R, Qiao Q, Lou JP, Gillespie P, Fotouhi N, Tilley J, Cohen N, Choudhry S, Cavallo G, Tannu SA, Ventre JD, Lavelle D, Tare NS, Oh H, Lamb M, Kurylko G, Hamid R, Wright MB, Pamidimukkala A, Egan T, Gubler U, Hoffman AF, Wei X, Li YL, O'Neil J, Marcano R, Pozzani K, Molinaro T, Santiago J, Singer L, Hargaden M, Moore D, Catala AR, Chao LC, Hermann G, Venkat R, Mancebo H, Renzetti LM.
J Med Chem (2010) 53 : 3502 -3516
PubMed 20380377 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.02 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1099323 1 7.42
CHEMBL1099326 1 7.15
CHEMBL1098560 1 6.94
CHEMBL1094348 1 6.89
CHEMBL1099330 1 6.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1099323 IC50 = 38.5 nM 7.42
CHEMBL1099326 IC50 = 71.0 nM 7.15
CHEMBL1098560 IC50 = 114.0 nM 6.94
CHEMBL1094348 IC50 = 129.0 nM 6.89
CHEMBL1099330 IC50 = 205.0 nM 6.69