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ChEMBL ligand: CHEMBL316966 (Camp, Cyclic Adenosine Monophosphate, cyclic AMP) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Rap guanine nucleotide exchange factor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2029197] [GtoPdb: 1292] [UniProtKB: O95398] | ||||||||
ChEMBL | 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 | B | 5.35 | pKd | 4500 | nM | Kd | J Med Chem (2020) 63: 4762-4775 [PMID:32297742] |
Rap guanine nucleotide exchange factor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2029198] [GtoPdb: 1293] [UniProtKB: Q8WZA2] | ||||||||
ChEMBL | Competitive inhibition of Epac2 using fluorescent nucleotide analog 8-NBD-cAMP by fluorescence analysis | B | 4.32 | pIC50 | 48000 | nM | IC50 | Bioorg. Med. Chem. Lett. (2012) 22: 4038-4043 [PMID:22607683] |
ChEMBL | Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay | B | 4.4 | pIC50 | 40000 | nM | IC50 | J. Med. Chem. (2013) 56: 952-962 [PMID:23286832] |
ChEMBL | Inhibition of EPAC2 (unknown origin) | B | 4.4 | pIC50 | 40000 | nM | IC50 | J. Med. Chem. (2014) 57: 3651-3665 [PMID:24256330] |
ChEMBL data shown on this page come from version 31:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]