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Assay Detail

CHEMBL1648902

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

Functional
Antagonist activity at prostaglandin D2 receptor in human LS174T cells assessed as inhibition of PGD2-induced cAMP accumulation after 15 mins by scintillation proximity assay
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type LS174T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin D2 receptor (CHEMBL4427)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Understanding DP receptor antagonism using a CoMSIA approach.
Mu L, Aguiar J, Ardati A, Cao B, Gardner CJ, Gillespy T, Harris K, Lim S, Marcus R, Morize I, Parkar A, Stefany D, Li Y, Vaz RJ, Cirovic DA.
Bioorg Med Chem Lett (2011) 21 : 66 -75
PubMed 21147533 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 60 8.12 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1644207 1 10.70
CHEMBL1644214 1 10.30
CHEMBL1644206 1 10.00
CHEMBL1644245 1 9.52
CHEMBL1644213 1 9.52
CHEMBL1644227 1 9.40
CHEMBL1644247 1 9.40
CHEMBL1644211 1 9.40
CHEMBL1644253 1 9.30
CHEMBL1644212 1 9.30
CHEMBL1644208 1 9.30
CHEMBL1644217 1 9.10
CHEMBL1644224 1 9.05
CHEMBL1644255 1 8.64
CHEMBL1644260 1 8.64
CHEMBL1644235 1 8.59
CHEMBL1644256 1 8.59
CHEMBL1644204 1 8.57
CHEMBL1644238 1 8.54
CHEMBL1644216 1 8.44
CHEMBL1644240 1 8.42
CHEMBL1644248 1 8.35
CHEMBL1644210 1 8.30
CHEMBL1644232 1 8.30
CHEMBL1644261 1 8.29
CHEMBL1644225 1 8.22
CHEMBL1644233 1 8.22
CHEMBL1644254 1 8.20
CHEMBL1644252 1 8.15
CHEMBL1644209 1 8.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1644207 IC50 = 0.01995 nM 10.70
CHEMBL1644214 IC50 = 0.05012 nM 10.30
CHEMBL1644206 IC50 = 0.1 nM 10.00
CHEMBL1644245 IC50 = 0.302 nM 9.52
CHEMBL1644213 IC50 = 0.302 nM 9.52
CHEMBL1644227 IC50 = 0.3981 nM 9.40
CHEMBL1644247 IC50 = 0.3981 nM 9.40
CHEMBL1644211 IC50 = 0.3981 nM 9.40
CHEMBL1644253 IC50 = 0.5012 nM 9.30
CHEMBL1644212 IC50 = 0.5012 nM 9.30
CHEMBL1644208 IC50 = 0.5012 nM 9.30
CHEMBL1644217 IC50 = 0.7943 nM 9.10
CHEMBL1644224 IC50 = 0.8913 nM 9.05
CHEMBL1644260 IC50 = 2.291 nM 8.64
CHEMBL1644255 IC50 = 2.291 nM 8.64
CHEMBL1644235 IC50 = 2.57 nM 8.59
CHEMBL1644256 IC50 = 2.57 nM 8.59
CHEMBL1644204 IC50 = 2.692 nM 8.57
CHEMBL1644238 IC50 = 2.884 nM 8.54
CHEMBL1644216 IC50 = 3.631 nM 8.44
CHEMBL1644240 IC50 = 3.802 nM 8.42
CHEMBL1644248 IC50 = 4.467 nM 8.35
CHEMBL1644210 IC50 = 5.012 nM 8.30
CHEMBL1644232 IC50 = 5.012 nM 8.30
CHEMBL1644261 IC50 = 5.129 nM 8.29
CHEMBL1644225 IC50 = 6.026 nM 8.22
CHEMBL1644233 IC50 = 6.026 nM 8.22
CHEMBL1644254 IC50 = 6.31 nM 8.20
CHEMBL1644252 IC50 = 7.079 nM 8.15
CHEMBL1644209 IC50 = 7.079 nM 8.15
CHEMBL1644258 IC50 = 7.244 nM 8.14
CHEMBL1644226 IC50 = 7.586 nM 8.12
CHEMBL1644234 IC50 = 7.762 nM 8.11
CHEMBL1644230 IC50 = 7.943 nM 8.10
CHEMBL1644239 IC50 = 8.128 nM 8.09
CHEMBL1644228 IC50 = 10.0 nM 8.00
CHEMBL1644259 IC50 = 10.96 nM 7.96
CHEMBL1644231 IC50 = 12.02 nM 7.92
CHEMBL1644257 IC50 = 12.88 nM 7.89
CHEMBL1644250 IC50 = 12.88 nM 7.89
CHEMBL1644246 IC50 = 14.13 nM 7.85
CHEMBL1644237 IC50 = 16.98 nM 7.77
CHEMBL1644241 IC50 = 22.91 nM 7.64
CHEMBL1641628 IC50 = 25.7 nM 7.59
CHEMBL1644222 IC50 = 32.36 nM 7.49
CHEMBL1644215 IC50 = 38.02 nM 7.42
CHEMBL1644223 IC50 = 40.74 nM 7.39
CHEMBL1644249 IC50 = 41.69 nM 7.38
CHEMBL1644251 IC50 = 43.65 nM 7.36
CHEMBL1644236 IC50 = 54.95 nM 7.26