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Assay Detail

CHEMBL1051055

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 CHO cells
17
Total Activities
17
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 Intermediate

Target

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

Publication

7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
Sandham DA, Adcock C, Bala K, Barker L, Brown Z, Dubois G, Budd D, Cox B, Fairhurst RA, Furegati M, Leblanc C, Manini J, Profit R, Reilly J, Stringer R, Schmidt A, Turner KL, Watson SJ, Willis J, Williams G, Wilson C.
Bioorg Med Chem Lett (2009) 19 : 4794 -4798
PubMed 19592244 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.82 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL563949 1 7.51
CHEMBL559316 1 7.46
CHEMBL559044 1 7.44
CHEMBL557662 1 7.37
CHEMBL557457 1 7.32
CHEMBL560279 1 7.28
CHEMBL562339 1 7.25
CHEMBL398126 1 7.23
CHEMBL361812 RAMATROBAN 4.0 1 7.14
CHEMBL561539 1 6.99
CHEMBL551274 1 6.80
CHEMBL549587 1 6.55
CHEMBL564002 1 6.42
CHEMBL561942 1 6.21
CHEMBL549793 1 5.93
CHEMBL565106 1 5.58
CHEMBL562593 1 5.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL563949 Ki = 31.0 nM 7.51
CHEMBL559316 Ki = 35.0 nM 7.46
CHEMBL559044 Ki = 36.0 nM 7.44
CHEMBL557662 Ki = 43.0 nM 7.37
CHEMBL557457 Ki = 48.0 nM 7.32
CHEMBL560279 Ki = 52.0 nM 7.28
CHEMBL562339 Ki = 56.0 nM 7.25
CHEMBL398126 Ki = 59.0 nM 7.23
CHEMBL361812 RAMATROBAN Ki = 73.0 nM 7.14
CHEMBL561539 Ki = 103.0 nM 6.99
CHEMBL551274 Ki = 158.0 nM 6.80
CHEMBL549587 Ki = 282.0 nM 6.55
CHEMBL564002 Ki = 377.0 nM 6.42
CHEMBL561942 Ki = 619.0 nM 6.21
CHEMBL549793 Ki = 1171.0 nM 5.93
CHEMBL565106 Ki = 2619.0 nM 5.58
CHEMBL562593 Ki = 3220.0 nM 5.49