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Assay Detail

CHEMBL709859

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

Binding
Binding affinity at leukotriene B4 receptor on intact human PMNs by displacement of [3H]LTB4.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid and related compounds: high affinity leukotriene B4 receptor antagonists.
Daines RA, Chambers PA, Eggleston DS, Foley JJ, Griswold DE, Haltiwanger RC, Jakas DR, Kingsbury WD, Martin LD, Pendrak I.
J Med Chem (1994) 37 : 3327 -3336
PubMed 7932560 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.89 9.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL292782 1 9.33
CHEMBL95453 1 9.00
CHEMBL419948 1 8.89
CHEMBL328712 1 8.70
CHEMBL422420 1 8.40
CHEMBL115658 1 8.32
CHEMBL325637 1 8.24
CHEMBL422598 1 8.15
CHEMBL325773 1 8.10
CHEMBL112972 1 8.04
CHEMBL112707 1 7.81
CHEMBL115040 1 7.55
CHEMBL325643 1 7.28
CHEMBL115362 1 7.10
CHEMBL420488 1 6.95
CHEMBL113146 1 6.79
CHEMBL326192 1 6.78
CHEMBL112169 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL292782 Ki = 0.47 nM 9.33
CHEMBL95453 Ki = 1.0 nM 9.00
CHEMBL419948 Ki = 1.3 nM 8.89
CHEMBL328712 Ki = 2.0 nM 8.70
CHEMBL422420 Ki = 4.0 nM 8.40
CHEMBL115658 Ki = 4.8 nM 8.32
CHEMBL325637 Ki = 5.7 nM 8.24
CHEMBL422598 Ki = 7.1 nM 8.15
CHEMBL325773 Ki = 8.0 nM 8.10
CHEMBL112972 Ki = 9.2 nM 8.04
CHEMBL112707 Ki = 15.4 nM 7.81
CHEMBL115040 Ki = 28.0 nM 7.55
CHEMBL325643 Ki = 53.0 nM 7.28
CHEMBL115362 Ki = 80.0 nM 7.10
CHEMBL420488 Ki = 112.0 nM 6.95
CHEMBL113146 Ki = 161.0 nM 6.79
CHEMBL326192 Ki = 167.0 nM 6.78
CHEMBL112169 Ki = 240.0 nM 6.62