cyclic AMP [Ligand Id: 2352] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL316966 (Camp, Cyclic Adenosine Monophosphate, cyclic AMP)
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  • CNGA2 in Rat [GtoPdb: 395] [UniProtKB: Q00195]
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  • CNGA3 in Human [GtoPdb: 396] [UniProtKB: Q16281]
  • CNGA3 in Rat [GtoPdb: 396]
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  • HCN1 in Mouse [GtoPdb: 400] [UniProtKB: O88704]
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  • HCN2 in Mouse [GtoPdb: 401] [UniProtKB: O88703]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]
CNGA2 in Rat [GtoPdb: 395] [UniProtKB: Q00195]
GtoPdb - - 4.34 pEC50 45700 nM EC50 J Neurosci (1999) 19: 5332-47 [PMID:10377344];
Neuron (1994) 13: 611-21 [PMID:7522482];
Proc Natl Acad Sci USA (1994) 91: 8890-4 [PMID:7522325];
Sci Signal (2012) 5: ra48 [PMID:22786723]
CNGA3 in Human [GtoPdb: 396] [UniProtKB: Q16281]
GtoPdb - - 2.88 pKd - - - FEBS Lett (1996) 393: 211-5 [PMID:8814292];
J Biol Chem (2003) 278: 24617-23 [PMID:12730238]
CNGA3 in Rat [GtoPdb: 396]
GtoPdb - - 3.6 pKd - - - J Neurophysiol (2001) 85: 2335-49 [PMID:11387380]
HCN1 in Mouse [GtoPdb: 400] [UniProtKB: O88704]
GtoPdb - - 7.2 pKd - - - J Gen Physiol (2001) 117: 491-504 [PMID:11331358];
J Gen Physiol (2001) 118: 237-50 [PMID:11524455]
HCN2 in Mouse [GtoPdb: 401] [UniProtKB: O88703]
GtoPdb - - 6.3 pKi - - - Nature (1998) 393: 587-91 [PMID:9634236]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]