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Assay Detail

CHEMBL878773

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Functional
In vitro inhibition of cAMP formation evoked by prostaglandin D2 receptor in human platelets
ChEMBL ↗
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prostaglandin D2 receptor (CHEMBL4427) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 1. Bicyclo[2.2.1]heptane derivatives.
Mitsumori S, Tsuri T, Honma T, Hiramatsu Y, Okada T, Hashizume H, Inagaki M, Arimura A, Yasui K, Asanuma F, Kishino J, Ohtani M.
J Med Chem (2003) 46 : 2436 -2445
PubMed 12773047 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 6.81 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL312182 — — 1 7.72
CHEMBL312715 — — 1 7.66
CHEMBL78904 — — 1 7.60
CHEMBL309443 — — 1 7.50
CHEMBL312707 — — 1 7.48
CHEMBL81185 — — 1 7.47
CHEMBL311199 — — 1 7.35
CHEMBL309987 — — 1 7.28
CHEMBL420398 — — 1 7.24
CHEMBL309835 — — 1 7.16
CHEMBL312697 — — 1 7.15
CHEMBL309752 — — 1 7.07
CHEMBL81600 — — 1 7.00
CHEMBL81768 — — 1 6.92
CHEMBL81751 — — 1 6.89
CHEMBL83269 — — 1 6.80
CHEMBL79669 — — 1 6.80
CHEMBL82426 — — 1 6.77
CHEMBL2114171 — — 1 6.75
CHEMBL312983 — — 1 6.75
CHEMBL79095 — — 1 6.75
CHEMBL82537 — — 1 6.75
CHEMBL79320 — — 1 6.72
CHEMBL420777 — — 1 6.70
CHEMBL311038 — — 1 6.70
CHEMBL82489 — — 1 6.68
CHEMBL310301 — — 1 6.68
CHEMBL310454 — — 1 6.66
CHEMBL310505 — — 1 6.60
CHEMBL310643 — — 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL312182 — IC50 = 19.0 nM 7.72
CHEMBL312715 — IC50 = 22.0 nM 7.66
CHEMBL78904 — IC50 = 25.0 nM 7.60
CHEMBL309443 — IC50 = 32.0 nM 7.50
CHEMBL312707 — IC50 = 33.0 nM 7.48
CHEMBL81185 — IC50 = 34.0 nM 7.47
CHEMBL311199 — IC50 = 45.0 nM 7.35
CHEMBL309987 — IC50 = 52.0 nM 7.28
CHEMBL420398 — IC50 = 57.0 nM 7.24
CHEMBL309835 — IC50 = 70.0 nM 7.16
CHEMBL312697 — IC50 = 71.0 nM 7.15
CHEMBL309752 — IC50 = 86.0 nM 7.07
CHEMBL81600 — IC50 = 100.0 nM 7.00
CHEMBL81768 — IC50 = 120.0 nM 6.92
CHEMBL81751 — IC50 = 130.0 nM 6.89
CHEMBL83269 — IC50 = 160.0 nM 6.80
CHEMBL79669 — IC50 = 160.0 nM 6.80
CHEMBL82426 — IC50 = 170.0 nM 6.77
CHEMBL2114171 — IC50 = 180.0 nM 6.75
CHEMBL312983 — IC50 = 180.0 nM 6.75
CHEMBL79095 — IC50 = 180.0 nM 6.75
CHEMBL82537 — IC50 = 180.0 nM 6.75
CHEMBL79320 — IC50 = 190.0 nM 6.72
CHEMBL420777 — IC50 = 200.0 nM 6.70
CHEMBL311038 — IC50 = 200.0 nM 6.70
CHEMBL82489 — IC50 = 210.0 nM 6.68
CHEMBL310301 — IC50 = 210.0 nM 6.68
CHEMBL310454 — IC50 = 220.0 nM 6.66
CHEMBL310505 — IC50 = 250.0 nM 6.60
CHEMBL310643 — IC50 = 260.0 nM 6.58
CHEMBL81804 — IC50 = 280.0 nM 6.55
CHEMBL83893 — IC50 = 280.0 nM 6.55
CHEMBL311105 — IC50 = 320.0 nM 6.50
CHEMBL432935 — IC50 = 320.0 nM 6.50
CHEMBL309999 — IC50 = 320.0 nM 6.50
CHEMBL430627 — IC50 = 330.0 nM 6.48
CHEMBL81050 — IC50 = 340.0 nM 6.47
CHEMBL311769 — IC50 = 350.0 nM 6.46
CHEMBL413523 — IC50 = 380.0 nM 6.42
CHEMBL79522 — IC50 = 390.0 nM 6.41
CHEMBL78939 — IC50 = 430.0 nM 6.37
CHEMBL79511 — IC50 = 450.0 nM 6.35
CHEMBL79260 — IC50 = 570.0 nM 6.24
CHEMBL312834 — IC50 = 650.0 nM 6.19
CHEMBL309847 — IC50 = 720.0 nM 6.14
CHEMBL309519 — IC50 > 1000.0 nM -
CHEMBL81757 — IC50 > 1000.0 nM -