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Assay Detail

CHEMBL888187

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

Binding
Displacement of [3H]PG2 from human CRTh2 receptor expressed in CHO cells
22
Total Activities
22
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

2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Sandham DA, Aldcroft C, Baettig U, Barker L, Beer D, Bhalay G, Brown Z, Dubois G, Budd D, Bidlake L, Campbell E, Cox B, Everatt B, Harrison D, Leblanc CJ, Manini J, Profit R, Stringer R, Thompson KS, Turner KL, Tweed MF, Walker C, Watson SJ, Whitebread S, Willis J, Williams G, Wilson C.
Bioorg Med Chem Lett (2007) 17 : 4347 -4350
PubMed 17531480 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.51 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL397650 1 7.70
CHEMBL398126 1 7.23
CHEMBL394497 1 7.12
CHEMBL246311 1 7.08
CHEMBL395134 1 7.05
CHEMBL429470 1 7.00
CHEMBL397842 1 6.82
CHEMBL245908 1 6.81
CHEMBL245700 1 6.64
CHEMBL247739 1 6.51
CHEMBL397651 1 6.45
CHEMBL246312 1 6.35
CHEMBL245701 1 6.11
CHEMBL247544 1 6.10
CHEMBL394496 1 5.70
CHEMBL247738 1 5.65
CHEMBL247131 1 5.48
CHEMBL245707 1 5.29
CHEMBL395930 1 -
CHEMBL247541 1 -
CHEMBL395643 1 -
CHEMBL394657 METAXON 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL397650 Ki = 20.0 nM 7.70
CHEMBL398126 Ki = 59.0 nM 7.23
CHEMBL394497 Ki = 75.0 nM 7.12
CHEMBL246311 Ki = 83.0 nM 7.08
CHEMBL395134 Ki = 90.0 nM 7.05
CHEMBL429470 Ki = 99.0 nM 7.00
CHEMBL397842 Ki = 150.0 nM 6.82
CHEMBL245908 Ki = 154.0 nM 6.81
CHEMBL245700 Ki = 230.0 nM 6.64
CHEMBL247739 Ki = 311.0 nM 6.51
CHEMBL397651 Ki = 353.0 nM 6.45
CHEMBL246312 Ki = 446.0 nM 6.35
CHEMBL245701 Ki = 782.0 nM 6.11
CHEMBL247544 Ki = 799.0 nM 6.10
CHEMBL394496 Ki = 1990.0 nM 5.70
CHEMBL247738 Ki = 2250.0 nM 5.65
CHEMBL247131 Ki = 3280.0 nM 5.48
CHEMBL245707 Ki = 5130.0 nM 5.29
CHEMBL395930 Ki > 10000.0 nM -
CHEMBL247541 Ki > 10000.0 nM -
CHEMBL395643 Ki > 10000.0 nM -
CHEMBL394657 METAXON Ki > 10000.0 nM -