Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4186525

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

Functional
Agonist activity at recombinant human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level measured at 3 secs time interval by fura-2-AM dye based fluorescence assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prostaglandin E2 receptor EP3 subtype (CHEMBL3710)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of a potent, well-balanced EP2/EP3 dual agonist.
Kinoshita A, Higashino M, Yoshida K, Aratani Y, Kakuuchi A, Hanada K, Takeda H, Naganawa A, Matsuya H, Ohmoto K.
Bioorg Med Chem (2018) 26 : 200 -214
PubMed 29203142 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 8.43 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3751951 1 9.15
CHEMBL4217198 1 9.10
CHEMBL4204996 1 9.04
CHEMBL4208379 1 9.00
CHEMBL4206444 1 8.57
CHEMBL4205480 1 8.52
CHEMBL4209929 1 8.48
CHEMBL4211120 1 8.47
CHEMBL4212770 1 8.46
CHEMBL4214346 1 8.06
CHEMBL4216182 1 7.80
CHEMBL4213312 1 7.50
CHEMBL4207054 1 7.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3751951 EC50 = 0.7 nM 9.15
CHEMBL4217198 EC50 = 0.8 nM 9.10
CHEMBL4204996 EC50 = 0.91 nM 9.04
CHEMBL4208379 EC50 = 1.0 nM 9.00
CHEMBL4206444 EC50 = 2.7 nM 8.57
CHEMBL4205480 EC50 = 3.0 nM 8.52
CHEMBL4209929 EC50 = 3.3 nM 8.48
CHEMBL4211120 EC50 = 3.4 nM 8.47
CHEMBL4212770 EC50 = 3.5 nM 8.46
CHEMBL4214346 EC50 = 8.8 nM 8.06
CHEMBL4216182 EC50 = 16.0 nM 7.80
CHEMBL4213312 EC50 = 32.0 nM 7.50
CHEMBL4207054 EC50 = 36.0 nM 7.44