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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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]