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Assay Detail

CHEMBL1936638

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

Binding
Displacement of [3H]PGD2 from human CRTh2 receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Plasma
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin D2 receptor 2 (CHEMBL5071)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism.
Wang Y, Fu Z, Schmitt M, Wang X, Shen W, Rickel E, Martin T, Budelsky A, Marshall D, Collins T, Tang HL, Medina JC, Liu JJ.
Bioorg Med Chem Lett (2012) 22 : 367 -370
PubMed 22119474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.63 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1933918 1 8.22
CHEMBL1933919 1 7.89
CHEMBL1933917 1 7.82
CHEMBL1933920 1 7.82
CHEMBL570653 1 7.80
CHEMBL589973 1 7.68
CHEMBL1933915 1 7.19
CHEMBL1933916 1 6.58
CHEMBL1933762 1 -
CHEMBL1933763 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1933918 IC50 = 6.0 nM 8.22
CHEMBL1933919 IC50 = 13.0 nM 7.89
CHEMBL1933917 IC50 = 15.0 nM 7.82
CHEMBL1933920 IC50 = 15.0 nM 7.82
CHEMBL570653 IC50 = 16.0 nM 7.80
CHEMBL589973 IC50 = 21.0 nM 7.68
CHEMBL1933915 IC50 = 65.0 nM 7.19
CHEMBL1933916 IC50 = 260.0 nM 6.58
CHEMBL1933762 IC50 - -
CHEMBL1933763 IC50 - -