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Assay Detail

CHEMBL1027714

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Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Prostaglandin E2 receptor EP2 subtype (CHEMBL4909)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of CP-533536: an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation.
Cameron KO, Lefker BA, Ke HZ, Li M, Zawistoski MP, Tjoa CM, Wright AS, DeNinno SL, Paralkar VM, Owen TA, Yu L, Thompson DD.
Bioorg Med Chem Lett (2009) 19 : 2075 -2078
PubMed 19250823 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 7.43 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559065 1 9.70
CHEMBL548 DINOPROSTONE 4.0 1 9.70
CHEMBL563646 EVATANEPAG 2.0 1 9.52
CHEMBL541517 1 8.96
CHEMBL541516 1 8.64
CHEMBL549870 1 7.46
CHEMBL562411 1 7.36
CHEMBL556333 1 7.32
CHEMBL556416 1 7.24
CHEMBL549461 1 7.03
CHEMBL559760 1 6.99
CHEMBL551951 1 6.87
CHEMBL549869 1 6.69
CHEMBL559561 1 6.39
CHEMBL550619 1 6.38
CHEMBL554823 1 6.37
CHEMBL558671 1 6.34
CHEMBL559820 1 6.23
CHEMBL562291 1 6.05
CHEMBL559955 1 -
CHEMBL549663 1 -
CHEMBL549530 1 -
CHEMBL562825 1 -
CHEMBL553468 1 -
CHEMBL550015 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559065 EC50 = 0.2 nM 9.70
CHEMBL548 DINOPROSTONE EC50 = 0.2 nM 9.70
CHEMBL563646 EVATANEPAG EC50 = 0.3 nM 9.52
CHEMBL541517 EC50 = 1.1 nM 8.96
CHEMBL541516 EC50 = 2.3 nM 8.64
CHEMBL549870 EC50 = 34.4 nM 7.46
CHEMBL562411 EC50 = 44.0 nM 7.36
CHEMBL556333 EC50 = 48.0 nM 7.32
CHEMBL556416 EC50 = 58.0 nM 7.24
CHEMBL549461 EC50 = 94.0 nM 7.03
CHEMBL559760 EC50 = 102.7 nM 6.99
CHEMBL551951 EC50 = 134.0 nM 6.87
CHEMBL549869 EC50 = 203.0 nM 6.69
CHEMBL559561 EC50 = 407.0 nM 6.39
CHEMBL550619 EC50 = 413.0 nM 6.38
CHEMBL554823 EC50 = 423.0 nM 6.37
CHEMBL558671 EC50 = 457.0 nM 6.34
CHEMBL559820 EC50 = 587.0 nM 6.23
CHEMBL562291 EC50 = 887.0 nM 6.05
CHEMBL559955 EC50 - -
CHEMBL549663 EC50 - -
CHEMBL549530 EC50 - -
CHEMBL562825 EC50 - -
CHEMBL553468 EC50 - -
CHEMBL550015 EC50 - -