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ChEMBL ligand: CHEMBL3260990 |
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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 human EPAC1 cAMP binding domain (149 to 318 residues) using aggregate form of compound by [15N-1H]HSQC spectroscopic analysis | B | 4.7 | pKd | 20000 | nM | Kd | J Med Chem (2019) 62: 5063-5079 [PMID:31074269] |
ChEMBL | Inhibition of 8-NBD-cAMP binding to human EPAC1 cAMP binding domain (149 to 318 residues) by fluorescence assay | B | 4.7 | pKd | 20000 | nM | Kd | J Med Chem (2019) 62: 5063-5079 [PMID:31074269] |
ChEMBL | Inhibition of recombinant C-terminal FLAG/HA-tagged EPAC1 (unknown origin) expressed in retrovirus infected human HeLaS3 cells assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal truncated Rap1B (1 to 167 residues)-Mant-GDP by spectrofluorometric analysis | B | 4.97 | pIC50 | 10800 | nM | IC50 | ACS Med Chem Lett (2016) 7: 460-464 [PMID:27190593] |
ChEMBL | Antagonist activity at EPAC1 (unknown origin) assessed as cAMP-induced guanine nucleotide exchange factor activity | B | 4.97 | pIC50 | 10800 | nM | IC50 | J Med Chem (2015) 58: 6033-6047 [PMID:26151319] |
ChEMBL | Antagonist activity at human recombinant EPAC1 assessed as inhibition of Rap1b-bGDP exchange activity | B | 4.97 | pIC50 | 10800 | nM | IC50 | J Med Chem (2015) 58: 6033-6047 [PMID:26151319] |
ChEMBL | Antagonist activity at recombinant human full length EPAC1 assessed as inhibition of EPAC1-mediated Rap1B (1 to 167 residues)-BODIPY GDP nucleotide exchange activity by 8-NBD-cAMP competition assay | B | 4.97 | pIC50 | 10800 | nM | IC50 | Eur J Med Chem (2017) 134: 62-71 [PMID:28399451] |
ChEMBL | Antagonist activity at recombinant full length EPAC1 (unknown origin) assessed as inhibition of cAMP-mediated Rap1b-BODIPY GDP nucleotide exchange activity | B | 5.04 | pIC50 | 9100 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 5163-5166 [PMID:29100797] |
GtoPdb | Measuring EPAC1-mediated guanine nucleotide exchange factor (GEF) activity. | - | 5.49 | pIC50 | 3200 | nM | IC50 | Mol Pharmacol (2013) 83: 122-8 [PMID:23066090] |
ChEMBL | Inhibition of EPAC1 (unknown origin) | B | 5.49 | pIC50 | 3200 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1633-1639 [PMID:28283242] |
ChEMBL | Inhibition of EPAC1 (unknown origin) assessed as cAMP-mediated GEF activity | B | 5.49 | pIC50 | 3200 | nM | IC50 | J Med Chem (2014) 57: 3651-3665 [PMID:24256330] |
Rap guanine nucleotide exchange factor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2029198] [GtoPdb: 1293] [UniProtKB: Q8WZA2] | ||||||||
ChEMBL | Displacement of 8-NBD-cAMP from EPAC2 (unknown origin) | B | 5.05 | pIC50 | 9000 | nM | IC50 | J Med Chem (2015) 58: 6033-6047 [PMID:26151319] |
GtoPdb | Measuring EPAC2-mediated guanine nucleotide exchange factor (GEF) activity. | - | 5.15 | pIC50 | 7000 | nM | IC50 |
Mol Pharmacol (2013) 83: 122-8 [PMID:23066090]; J Med Chem (2014) 57: 3651-65 [PMID:24256330] |
ChEMBL | Displacement of 8-NBD-cAMP from EPAC2 (unknown origin) by fluorescence plate reader analysis | B | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (2014) 57: 3651-3665 [PMID:24256330] |
ChEMBL | Inhibition of EPAC2 (unknown origin) | B | 5.15 | pIC50 | 7000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1633-1639 [PMID:28283242] |
ChEMBL | Antagonist activity at EPAC2 (unknown origin) assessed as cAMP-induced guanine nucleotide exchange factor activity | B | 5.36 | pIC50 | 4400 | nM | IC50 | J Med Chem (2015) 58: 6033-6047 [PMID:26151319] |
ChEMBL | Inhibition of recombinant C-terminal FLAG/HA-tagged EPAC2 (unknown origin) expressed in retrovirus infected human HeLaS3 cells assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal truncated Rap1B (1 to 167 residues)-Mant-GDP by spectrofluorometric analysis | B | 5.36 | pIC50 | 4400 | nM | IC50 | ACS Med Chem Lett (2016) 7: 460-464 [PMID:27190593] |
ChEMBL | Antagonist activity at recombinant full length EPAC2 (unknown origin) assessed as inhibition of cAMP-mediated Rap1b-BODIPY GDP nucleotide exchange activity | B | 5.36 | pIC50 | 4400 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 5163-5166 [PMID:29100797] |
Rap guanine nucleotide exchange factor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3593151] [GtoPdb: 1293] [UniProtKB: Q9EQZ6] | ||||||||
ChEMBL | Displacement of 8-NBD-cAMP from mouse recombinant EPAC2 by fluorescence assay | B | 5.05 | pIC50 | 8900 | nM | IC50 | J Med Chem (2015) 58: 6033-6047 [PMID:26151319] |
ChEMBL | Antagonist activity at mouse EPAC2 assessed as inhibition of EPAC2-mediated Rap1B (1 to 167 residues)-BODIPY GDP nucleotide exchange activity by 8-NBD-cAMP competition assay | B | 5.36 | pIC50 | 4400 | nM | IC50 | Eur J Med Chem (2017) 134: 62-71 [PMID:28399451] |
Serum albumin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3253] [UniProtKB: P02768] | ||||||||
ChEMBL | Displacement of dansylated arginine from human serum albumin by fluorescence assay | B | 6.64 | pKd | 230 | nM | Kd | J Med Chem (2019) 62: 5063-5079 [PMID:31074269] |
ChEMBL | Displacement of dansylated phenylalanine from human serum albumin by fluorescence assay | B | 7 | pKd | 99 | nM | Kd | J Med Chem (2019) 62: 5063-5079 [PMID:31074269] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]