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Assay Detail

CHEMBL664841

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

Binding
Displacement of [3H]LTD4 from Cysteinyl leukotriene D4 receptor in guinea pig lung membranes
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and structure-activity relationships of carboxylated chalcones: a novel series of CysLT1 (LTD4) receptor antagonists.
Zwaagstra ME, Timmerman H, Tamura M, Tohma T, Wada Y, Onogi K, Zhang MQ.
J Med Chem (1997) 40 : 1075 -1089
PubMed 9089329 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 48 6.39 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL21333 PRANLUKAST 4.0 1 9.00
CHEMBL11905 1 8.18
CHEMBL11899 1 7.85
CHEMBL12018 1 7.68
CHEMBL11508 1 7.58
CHEMBL11687 1 7.51
CHEMBL11870 1 7.35
CHEMBL11625 1 6.98
CHEMBL11921 1 6.98
CHEMBL11745 1 6.85
CHEMBL11509 1 6.84
CHEMBL12212 1 6.76
CHEMBL269220 1 6.73
CHEMBL269416 1 6.71
CHEMBL11732 1 6.70
CHEMBL11796 1 6.69
CHEMBL11920 1 6.69
CHEMBL11533 1 6.68
CHEMBL11349 1 6.68
CHEMBL11895 1 6.68
CHEMBL273727 1 6.63
CHEMBL11902 1 6.62
CHEMBL11609 1 6.52
CHEMBL11550 1 6.51
CHEMBL11793 1 6.46
CHEMBL11532 1 6.45
CHEMBL11782 1 6.40
CHEMBL11950 1 6.38
CHEMBL11914 1 6.35
CHEMBL11791 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL21333 PRANLUKAST Kd = 1.0 nM 9.00
CHEMBL11905 Kd = 6.6 nM 8.18
CHEMBL11899 Kd = 14.0 nM 7.85
CHEMBL12018 Kd = 21.0 nM 7.68
CHEMBL11508 Kd = 26.0 nM 7.58
CHEMBL11687 Kd = 31.0 nM 7.51
CHEMBL11870 Kd = 45.0 nM 7.35
CHEMBL11625 Kd = 105.0 nM 6.98
CHEMBL11921 Kd = 104.0 nM 6.98
CHEMBL11745 Kd = 140.0 nM 6.85
CHEMBL11509 Kd = 143.0 nM 6.84
CHEMBL12212 Kd = 175.0 nM 6.76
CHEMBL269220 Kd = 188.0 nM 6.73
CHEMBL269416 Kd = 196.0 nM 6.71
CHEMBL11732 Kd = 200.0 nM 6.70
CHEMBL11796 Kd = 204.0 nM 6.69
CHEMBL11920 Kd = 205.0 nM 6.69
CHEMBL11533 Kd = 209.0 nM 6.68
CHEMBL11349 Kd = 207.0 nM 6.68
CHEMBL11895 Kd = 208.0 nM 6.68
CHEMBL273727 Kd = 233.0 nM 6.63
CHEMBL11902 Kd = 239.0 nM 6.62
CHEMBL11609 Kd = 300.0 nM 6.52
CHEMBL11550 Kd = 307.0 nM 6.51
CHEMBL11793 Kd = 346.0 nM 6.46
CHEMBL11532 Kd = 357.0 nM 6.45
CHEMBL11782 Kd = 396.0 nM 6.40
CHEMBL11950 Kd = 415.0 nM 6.38
CHEMBL11914 Kd = 449.0 nM 6.35
CHEMBL11791 Kd = 450.0 nM 6.35
CHEMBL11606 Kd = 527.0 nM 6.28
CHEMBL11718 Kd = 585.0 nM 6.23
CHEMBL276879 Kd = 609.0 nM 6.21
CHEMBL273415 Kd = 732.0 nM 6.13
CHEMBL12143 Kd = 828.0 nM 6.08
CHEMBL12036 Kd = 928.0 nM 6.03
CHEMBL267475 FPL-55712 Kd = 1122.0 nM 5.95
CHEMBL11822 Kd = 1210.0 nM 5.92
CHEMBL11785 Kd = 1700.0 nM 5.77
CHEMBL11244 Kd = 2100.0 nM 5.68
CHEMBL11786 Kd = 4310.0 nM 5.37
CHEMBL418156 Kd = 8850.0 nM 5.05
CHEMBL273899 Kd = 10500.0 nM 4.98
CHEMBL12287 Kd = 11100.0 nM 4.96
CHEMBL11521 Kd = 14800.0 nM 4.83
CHEMBL11778 Kd = 19200.0 nM 4.72
CHEMBL12073 Kd = 33500.0 nM 4.47
CHEMBL11911 Kd = 62400.0 nM 4.21