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Assay Detail

CHEMBL666490

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

Binding
Inhibition constant for displacement of [3H]LTD4 on guinea pig lung parenchymal membranes.
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Lung parenchyma
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Cysteinyl leukotriene receptor (CHEMBL2094254)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Evolution of a series of peptidoleukotriene antagonists: synthesis and structure/activity relationships of 1,3,5-substituted indoles and indazoles.
Matassa VG, Maduskuie TP, Shapiro HS, Hesp B, Snyder DW, Aharony D, Krell RD, Keith RA.
J Med Chem (1990) 33 : 1781 -1790
PubMed 2342072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 8.62 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL299837 1 10.00
CHEMBL48927 1 9.70
CHEMBL51585 1 9.60
CHEMBL299093 1 9.60
CHEMBL297952 1 9.52
CHEMBL49944 1 9.52
CHEMBL300096 1 9.52
CHEMBL50562 1 9.52
CHEMBL412056 1 9.52
CHEMBL296821 1 9.52
CHEMBL301616 1 9.30
CHEMBL51580 1 9.15
CHEMBL48435 1 9.10
CHEMBL49566 1 8.85
CHEMBL51289 1 8.25
CHEMBL51239 1 8.17
CHEMBL51061 1 8.00
CHEMBL49981 1 7.28
CHEMBL50364 1 7.24
CHEMBL430967 1 7.17
CHEMBL300943 1 7.16
CHEMBL297014 1 7.15
CHEMBL52260 1 7.08
CHEMBL300906 1 6.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL299837 Ki = 0.1 nM 10.00
CHEMBL48927 Ki = 0.2 nM 9.70
CHEMBL51585 Ki = 0.25 nM 9.60
CHEMBL299093 Ki = 0.25 nM 9.60
CHEMBL297952 Ki = 0.3 nM 9.52
CHEMBL49944 Ki = 0.3 nM 9.52
CHEMBL300096 Ki = 0.3 nM 9.52
CHEMBL50562 Ki = 0.3 nM 9.52
CHEMBL412056 Ki = 0.3 nM 9.52
CHEMBL296821 Ki = 0.3 nM 9.52
CHEMBL301616 Ki = 0.5 nM 9.30
CHEMBL51580 Ki = 0.7 nM 9.15
CHEMBL48435 Ki = 0.8 nM 9.10
CHEMBL49566 Ki = 1.4 nM 8.85
CHEMBL51289 Ki = 5.6 nM 8.25
CHEMBL51239 Ki = 6.8 nM 8.17
CHEMBL51061 Ki = 10.0 nM 8.00
CHEMBL49981 Ki = 53.0 nM 7.28
CHEMBL50364 Ki = 57.0 nM 7.24
CHEMBL430967 Ki = 67.0 nM 7.17
CHEMBL300943 Ki = 70.0 nM 7.16
CHEMBL297014 Ki = 71.0 nM 7.15
CHEMBL52260 Ki = 84.0 nM 7.08
CHEMBL300906 Ki = 132.0 nM 6.88