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Assay Detail

CHEMBL2039538

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

Binding
Displacement of [3HPGD2 from human CRTH2 receptor expressed in CHO cell membrane after 90 mins by scintillation proximity assay
ChEMBL ↗
57
Total Activities
57
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 Autocuration

Target

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

Publication

Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids.
Crosignani S, Jorand-Lebrun C, Campbell G, Prêtre A, Grippi-Vallotton T, Quattropani A, Bouscary-Desforges G, Bombrun A, Missotten M, Humbert Y, Frémaux C, Pâquet M, El Harkani K, Bradshaw CG, Cleva C, Abla N, Daff H, Schott O, Pittet PA, Arrighi JF, Gaudet M, Johnson Z.
ACS Med Chem Lett (2011) 2 : 938 -942
PubMed 24900284 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 57 7.58 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2036225 — — 1 9.05
CHEMBL2036207 — — 1 8.70
CHEMBL2036224 — — 1 8.66
CHEMBL2036211 — — 1 8.62
CHEMBL2036226 — — 1 8.60
CHEMBL2036025 — — 1 8.52
CHEMBL2036028 — — 1 8.52
CHEMBL2036220 — — 1 8.51
CHEMBL2036222 — — 1 8.49
CHEMBL2036016 — — 1 8.48
CHEMBL2036029 — — 1 8.44
CHEMBL2036228 — — 1 8.40
CHEMBL2036212 — — 1 8.35
CHEMBL2036206 — — 1 8.31
CHEMBL2036216 — — 1 8.28
CHEMBL2036223 — — 1 8.27
CHEMBL2036205 — — 1 8.25
CHEMBL2036210 — — 1 8.24
CHEMBL2036030 — — 1 8.19
CHEMBL2036213 — — 1 8.16
CHEMBL2036203 — — 1 8.15
CHEMBL2036036 — — 1 8.15
CHEMBL2036027 — — 1 8.12
CHEMBL2036214 — — 1 8.11
CHEMBL2036026 — — 1 8.09
CHEMBL2036015 — — 1 8.00
CHEMBL2036204 — — 1 7.96
CHEMBL2036202 — — 1 7.92
CHEMBL2036221 — — 1 7.77
CHEMBL2036229 — — 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2036225 — Ki = 0.9 nM 9.05
CHEMBL2036207 — Ki = 2.0 nM 8.70
CHEMBL2036224 — Ki = 2.2 nM 8.66
CHEMBL2036211 — Ki = 2.4 nM 8.62
CHEMBL2036226 — Ki = 2.5 nM 8.60
CHEMBL2036025 — Ki = 3.0 nM 8.52
CHEMBL2036028 — Ki = 3.0 nM 8.52
CHEMBL2036220 — Ki = 3.1 nM 8.51
CHEMBL2036222 — Ki = 3.2 nM 8.49
CHEMBL2036016 — Ki = 3.3 nM 8.48
CHEMBL2036029 — Ki = 3.6 nM 8.44
CHEMBL2036228 — Ki = 4.0 nM 8.40
CHEMBL2036212 — Ki = 4.5 nM 8.35
CHEMBL2036206 — Ki = 4.9 nM 8.31
CHEMBL2036216 — Ki = 5.2 nM 8.28
CHEMBL2036223 — Ki = 5.4 nM 8.27
CHEMBL2036205 — Ki = 5.6 nM 8.25
CHEMBL2036210 — Ki = 5.7 nM 8.24
CHEMBL2036030 — Ki = 6.4 nM 8.19
CHEMBL2036213 — Ki = 6.9 nM 8.16
CHEMBL2036203 — Ki = 7.0 nM 8.15
CHEMBL2036036 — Ki = 7.1 nM 8.15
CHEMBL2036027 — Ki = 7.6 nM 8.12
CHEMBL2036214 — Ki = 7.7 nM 8.11
CHEMBL2036026 — Ki = 8.2 nM 8.09
CHEMBL2036015 — Ki = 10.0 nM 8.00
CHEMBL2036204 — Ki = 11.0 nM 7.96
CHEMBL2036202 — Ki = 12.0 nM 7.92
CHEMBL2036221 — Ki = 17.0 nM 7.77
CHEMBL2036229 — Ki = 17.0 nM 7.77
CHEMBL2036035 — Ki = 18.0 nM 7.75
CHEMBL2036215 — Ki = 19.0 nM 7.72
CHEMBL2036218 — Ki = 22.0 nM 7.66
CHEMBL2036217 — Ki = 26.0 nM 7.58
CHEMBL2036227 — Ki = 28.0 nM 7.55
CHEMBL2036018 — Ki = 39.0 nM 7.41
CHEMBL2036201 — Ki = 42.0 nM 7.38
CHEMBL2036024 — Ki = 44.0 nM 7.36
CHEMBL2036198 — Ki = 45.0 nM 7.35
CHEMBL2036017 — Ki = 50.0 nM 7.30
CHEMBL2036200 — Ki = 56.0 nM 7.25
CHEMBL2036219 — Ki = 69.0 nM 7.16
CHEMBL2036209 — Ki = 110.0 nM 6.96
CHEMBL2036199 — Ki = 130.0 nM 6.89
CHEMBL2036014 — Ki = 140.0 nM 6.85
CHEMBL2036023 — Ki = 220.0 nM 6.66
CHEMBL2036208 — Ki = 220.0 nM 6.66
CHEMBL2036019 — Ki = 330.0 nM 6.48
CHEMBL2036022 — Ki = 360.0 nM 6.44
CHEMBL2036034 — Ki = 580.0 nM 6.24