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Assay Detail

CHEMBL871676

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Binding
Binding affinity towards human CRTH2 receptor expressed in CHO cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2.
Armer RE, Ashton MR, Boyd EA, Brennan CJ, Brookfield FA, Gazi L, Gyles SL, Hay PA, Hunter MG, Middlemiss D, Whittaker M, Xue L, Pettipher R.
J Med Chem (2005) 48 : 6174 -6177
PubMed 16190744 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.83 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370606 1 9.10
CHEMBL373294 1 7.72
CHEMBL199040 1 7.54
CHEMBL196707 1 7.17
CHEMBL370257 1 7.15
CHEMBL196617 1 6.65
CHEMBL197398 1 6.60
CHEMBL364299 1 6.52
CHEMBL193753 1 6.34
CHEMBL194918 1 6.20
CHEMBL194019 1 5.53
CHEMBL18797 SULINDAC SULFIDE -1.0 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370606 Ki = 0.8 nM 9.10
CHEMBL373294 Ki = 19.0 nM 7.72
CHEMBL199040 Ki = 29.0 nM 7.54
CHEMBL196707 Ki = 68.0 nM 7.17
CHEMBL370257 Ki = 71.0 nM 7.15
CHEMBL196617 Ki = 225.0 nM 6.65
CHEMBL197398 Ki = 250.0 nM 6.60
CHEMBL364299 Ki = 299.0 nM 6.52
CHEMBL193753 Ki = 457.0 nM 6.34
CHEMBL194918 Ki = 634.0 nM 6.20
CHEMBL194019 Ki = 2979.0 nM 5.53
CHEMBL18797 SULINDAC SULFIDE Ki = 3500.0 nM 5.46