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Assay Detail

CHEMBL664974

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

Binding
In vitro affinity for CysLT1 receptors on guinea pig lung membranes, measured by displacement of [3H]LTD4.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Lung
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cysteinyl leukotriene receptor 1 (CHEMBL5645)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis and structure-activity relationships of carboxyflavones as structurally rigid CysLT1 (LTD4) receptor antagonists.
Zwaagstra ME, Timmerman H, van de Stolpe AC, de Kanter FJ, Tamura M, Wada Y, Zhang MQ.
J Med Chem (1998) 41 : 1428 -1438
PubMed 9554876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 23 6.67 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL416769 1 7.96
CHEMBL33729 1 7.92
CHEMBL34835 1 7.89
CHEMBL32136 1 7.77
CHEMBL33871 1 7.77
CHEMBL284624 1 7.77
CHEMBL32138 1 7.51
CHEMBL287559 1 7.10
CHEMBL34740 1 7.00
CHEMBL284730 1 6.90
CHEMBL33331 1 6.68
CHEMBL32764 1 6.57
CHEMBL33607 1 6.51
CHEMBL285994 1 6.42
CHEMBL33329 1 6.39
CHEMBL34507 1 6.30
CHEMBL33294 1 6.28
CHEMBL417135 1 5.96
CHEMBL34177 1 5.95
CHEMBL33276 1 5.76
CHEMBL32944 1 5.76
CHEMBL33228 1 4.96
CHEMBL286797 1 4.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL416769 Kd = 11.0 nM 7.96
CHEMBL33729 Kd = 12.0 nM 7.92
CHEMBL34835 Kd = 13.0 nM 7.89
CHEMBL32136 Kd = 17.0 nM 7.77
CHEMBL33871 Kd = 17.0 nM 7.77
CHEMBL284624 Kd = 17.0 nM 7.77
CHEMBL32138 Kd = 31.0 nM 7.51
CHEMBL287559 Kd = 79.0 nM 7.10
CHEMBL34740 Kd = 101.0 nM 7.00
CHEMBL284730 Kd = 127.0 nM 6.90
CHEMBL33331 Kd = 210.0 nM 6.68
CHEMBL32764 Kd = 270.0 nM 6.57
CHEMBL33607 Kd = 307.0 nM 6.51
CHEMBL285994 Kd = 382.0 nM 6.42
CHEMBL33329 Kd = 408.0 nM 6.39
CHEMBL34507 Kd = 504.0 nM 6.30
CHEMBL33294 Kd = 526.0 nM 6.28
CHEMBL417135 Kd = 1100.0 nM 5.96
CHEMBL34177 Kd = 1130.0 nM 5.95
CHEMBL33276 Kd = 1750.0 nM 5.76
CHEMBL32944 Kd = 1730.0 nM 5.76
CHEMBL33228 Kd = 11000.0 nM 4.96
CHEMBL286797 Kd = 55000.0 nM 4.26