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Assay Detail

CHEMBL4605939

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

Binding
Binding affinity to GST-tagged human EPAC1 CNBD (149 to 318 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by 8-NBD-cAMP based competitive fluorescence assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Rap guanine nucleotide exchange factor 3 (CHEMBL2029197)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Mechanism of Action of an EPAC1-Selective Competitive Partial Agonist.
Shao H, Mohamed H, Boulton S, Huang J, Wang P, Chen H, Zhou J, Luchowska-Stańska U, Jentsch NG, Armstrong AL, Magolan J, Yarwood S, Melacini G.
J Med Chem (2020) 63 : 4762 -4775
PubMed 32297742 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 5.27 5.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL316966 CYCLIC ADENOSINE MONOPHOSPHATE 1 5.35
CHEMBL4534834 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL316966 CYCLIC ADENOSINE MONOPHOSPHATE Kd = 4500.0 nM 5.35
CHEMBL4534834 Kd = 6600.0 nM 5.18