ChEMBL ligand: CHEMBL3260990
Rap guanine nucleotide exchange factor 3 in Human [ChEMBL: CHEMBL2029197] [GtoPdb: 1292] [UniProtKB: O95398] There should be some charts here, you may need to enable JavaScript!
Rap guanine nucleotide exchange factor 4 in Human [ChEMBL: CHEMBL2029198] [GtoPdb: 1293] [UniProtKB: Q8WZA2] Rap guanine nucleotide exchange factor 4 in Mouse [ChEMBL: CHEMBL3593151] [GtoPdb: 1293] [UniProtKB: Q9EQZ6] There should be some charts here, you may need to enable JavaScript!
Serum albumin in Human [ChEMBL: CHEMBL3253] [UniProtKB: P02768] There should be some charts here, you may need to enable JavaScript!

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 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 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]