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Compile Data Set for Download or QSAR

Found 98 hits Enz. Inhib. hit(s) with Target = 'Rap guanine nucleotide exchange factor 4' AND taxid = 9606   
Target
(Institution)
LigandTarget
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50425531
PNG
(CHEMBL2313646)
Show SMILES Cc1cc(C)n(c1)S(=O)(=O)c1c(C)cc(C)cc1C
Show InChI InChI=1S/C15H19NO2S/c1-10-6-12(3)15(13(4)7-10)19(17,18)16-9-11(2)8-14(16)5/h6-9H,1-5H3
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n/an/a 300n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay


J Med Chem 56: 952-62 (2013)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175143
PNG
(CHEMBL3809313)
Show SMILES Cc1cc(C)c(Nc2c(C)cc(C)cc2C)c(C)c1
Show InChI InChI=1S/C18H23N/c1-11-7-13(3)17(14(4)8-11)19-18-15(5)9-12(2)10-16(18)6/h7-10,19H,1-6H3
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n/an/a 400n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175225
PNG
(CHEMBL3808606)
Show SMILES Cc1cc(C)c(Nc2ccc(Cl)c(c2)C(F)(F)F)c(C)c1
Show InChI InChI=1S/C16H15ClF3N/c1-9-6-10(2)15(11(3)7-9)21-12-4-5-14(17)13(8-12)16(18,19)20/h4-8,21H,1-3H3
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n/an/a 400n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50425555
PNG
(CHEMBL2313653)
Show SMILES Cc1ccc(cc1)S(=O)(=O)c1c(C)cc(C)cc1C
Show InChI InChI=1S/C16H18O2S/c1-11-5-7-15(8-6-11)19(17,18)16-13(3)9-12(2)10-14(16)4/h5-10H,1-4H3
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n/an/a 400n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of EPAC2 (unknown origin)


J Med Chem 57: 3651-65 (2014)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50425541
PNG
(CHEMBL2313637)
Show SMILES Cc1cc(C)c(Nc2cc(Cl)ccc2Cl)c(C)c1
Show InChI InChI=1S/C15H15Cl2N/c1-9-6-10(2)15(11(3)7-9)18-14-8-12(16)4-5-13(14)17/h4-8,18H,1-3H3
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n/an/a 400n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay


J Med Chem 56: 952-62 (2013)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175226
PNG
(CHEMBL3808936)
Show SMILES Cc1cc(C)c(Nc2cccc(Cl)c2C)c(C)c1
Show InChI InChI=1S/C16H18ClN/c1-10-8-11(2)16(12(3)9-10)18-15-7-5-6-14(17)13(15)4/h5-9,18H,1-4H3
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n/an/a 500n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175266
PNG
(CHEMBL3808997)
Show SMILES Cc1cc(C)c(Nc2cc(Cl)cc(c2)C(F)(F)F)c(C)c1
Show InChI InChI=1S/C16H15ClF3N/c1-9-4-10(2)15(11(3)5-9)21-14-7-12(16(18,19)20)6-13(17)8-14/h4-8,21H,1-3H3
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n/an/a 500n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50425555
PNG
(CHEMBL2313653)
Show SMILES Cc1ccc(cc1)S(=O)(=O)c1c(C)cc(C)cc1C
Show InChI InChI=1S/C16H18O2S/c1-11-5-7-15(8-6-11)19(17,18)16-13(3)9-12(2)10-14(16)4/h5-10H,1-4H3
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n/an/a 500n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay


J Med Chem 56: 952-62 (2013)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50425539
PNG
(CHEMBL2313639)
Show SMILES CCc1cccn1S(=O)(=O)c1c(C)cc(C)cc1C
Show InChI InChI=1S/C15H19NO2S/c1-5-14-7-6-8-16(14)19(17,18)15-12(3)9-11(2)10-13(15)4/h6-10H,5H2,1-4H3
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n/an/a 500n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay


J Med Chem 56: 952-62 (2013)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50011368
PNG
(CHEMBL3260989)
Show SMILES [I-].COCCC[n+]1c(C)csc1Nc1c(C)cc(C)cc1C
Show InChI InChI=1S/C17H24N2OS.HI/c1-12-9-13(2)16(14(3)10-12)18-17-19(7-6-8-20-5)15(4)11-21-17;/h9-11H,6-8H2,1-5H3;1H
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n/an/a 600n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of EPAC2 (unknown origin)


J Med Chem 57: 3651-65 (2014)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175100
PNG
(CHEMBL3809121)
Show SMILES Cc1cc(C)c(Nc2cc(cc(c2)C(F)(F)F)C(F)(F)F)c(C)c1
Show InChI InChI=1S/C17H15F6N/c1-9-4-10(2)15(11(3)5-9)24-14-7-12(16(18,19)20)6-13(8-14)17(21,22)23/h4-8,24H,1-3H3
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n/an/a 600n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50425554
PNG
(CHEMBL2313654)
Show SMILES Cc1cc(C)c(c(C)c1)S(=O)(=O)c1cc(C)c(C)cc1C
Show InChI InChI=1S/C18H22O2S/c1-11-7-15(5)18(16(6)8-11)21(19,20)17-10-13(3)12(2)9-14(17)4/h7-10H,1-6H3
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n/an/a 700n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay


J Med Chem 56: 952-62 (2013)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175228
PNG
(CHEMBL3808792)
Show SMILES Cc1cc(C)c(Nc2c(C)cc(Cl)cc2Cl)c(C)c1
Show InChI InChI=1S/C16H17Cl2N/c1-9-5-10(2)15(11(3)6-9)19-16-12(4)7-13(17)8-14(16)18/h5-8,19H,1-4H3
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n/an/a 700n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50425542
PNG
(CHEMBL2313636)
Show SMILES Cc1cc(C)c(Nc2cc(Cl)cc(Cl)c2)c(C)c1
Show InChI InChI=1S/C15H15Cl2N/c1-9-4-10(2)15(11(3)5-9)18-14-7-12(16)6-13(17)8-14/h4-8,18H,1-3H3
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n/an/a 900n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay


J Med Chem 56: 952-62 (2013)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175273
PNG
(CHEMBL3808989)
Show SMILES Cc1cc(C)c(Nc2cccc(C)c2C)c(C)c1
Show InChI InChI=1S/C17H21N/c1-11-9-13(3)17(14(4)10-11)18-16-8-6-7-12(2)15(16)5/h6-10,18H,1-5H3
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n/an/a 1.00E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175225
PNG
(CHEMBL3808606)
Show SMILES Cc1cc(C)c(Nc2ccc(Cl)c(c2)C(F)(F)F)c(C)c1
Show InChI InChI=1S/C16H15ClF3N/c1-9-6-10(2)15(11(3)7-9)21-12-4-5-14(17)13(8-12)16(18,19)20/h4-8,21H,1-3H3
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n/an/a 1.00E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of EPAC2 (unknown origin) assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal tru...


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175227
PNG
(CHEMBL3809399)
Show SMILES Cc1cc(C)c(Nc2ccc(Cl)c(Cl)c2)c(C)c1
Show InChI InChI=1S/C15H15Cl2N/c1-9-6-10(2)15(11(3)7-9)18-12-4-5-13(16)14(17)8-12/h4-8,18H,1-3H3
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n/an/a 1.10E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175270
PNG
(CHEMBL3808484)
Show SMILES Cc1cc(C)c(Nc2cc(Cl)c(Cl)c(Cl)c2)c(C)c1
Show InChI InChI=1S/C15H14Cl3N/c1-8-4-9(2)15(10(3)5-8)19-11-6-12(16)14(18)13(17)7-11/h4-7,19H,1-3H3
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n/an/a 1.10E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM89901
PNG
(1-(2,4,6-Trimethyl-benzenesulfonyl)-1H-indole | 1-...)
Show SMILES Cc1cc(C)c(c(C)c1)S(=O)(=O)n1ccc2ccccc12
Show InChI InChI=1S/C17H17NO2S/c1-12-10-13(2)17(14(3)11-12)21(19,20)18-9-8-15-6-4-5-7-16(15)18/h4-11H,1-3H3
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n/an/a 1.20E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay


J Med Chem 56: 952-62 (2013)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175100
PNG
(CHEMBL3809121)
Show SMILES Cc1cc(C)c(Nc2cc(cc(c2)C(F)(F)F)C(F)(F)F)c(C)c1
Show InChI InChI=1S/C17H15F6N/c1-9-4-10(2)15(11(3)5-9)24-14-7-12(16(18,19)20)6-13(8-14)17(21,22)23/h4-8,24H,1-3H3
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n/an/a 1.30E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of EPAC2 (unknown origin) assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal tru...


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50425532
PNG
(CHEMBL2313645)
Show SMILES CCc1cccn1S(=O)(=O)c1ccc(C)cc1C
Show InChI InChI=1S/C14H17NO2S/c1-4-13-6-5-9-15(13)18(16,17)14-8-7-11(2)10-12(14)3/h5-10H,4H2,1-3H3
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n/an/a 1.30E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay


J Med Chem 56: 952-62 (2013)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175265
PNG
(CHEMBL3808689)
Show SMILES Cc1cc(C)c(Nc2cc(Cl)ccc2C)c(C)c1
Show InChI InChI=1S/C16H18ClN/c1-10-7-12(3)16(13(4)8-10)18-15-9-14(17)6-5-11(15)2/h5-9,18H,1-4H3
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n/an/a 1.40E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175267
PNG
(CHEMBL3809943)
Show SMILES Cc1cc(C)c(Nc2cccc(Br)c2)c(C)c1
Show InChI InChI=1S/C15H16BrN/c1-10-7-11(2)15(12(3)8-10)17-14-6-4-5-13(16)9-14/h4-9,17H,1-3H3
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n/an/a 1.50E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175268
PNG
(CHEMBL3809058)
Show SMILES Cc1cc(C)c(Nc2ccc(Br)cc2)c(C)c1
Show InChI InChI=1S/C15H16BrN/c1-10-8-11(2)15(12(3)9-10)17-14-6-4-13(16)5-7-14/h4-9,17H,1-3H3
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n/an/a 1.60E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175070
PNG
(CHEMBL3809465)
Show SMILES Cc1cc(C)cc(Nc2c(C)cc(C)cc2C)c1
Show InChI InChI=1S/C17H21N/c1-11-6-12(2)10-16(9-11)18-17-14(4)7-13(3)8-15(17)5/h6-10,18H,1-5H3
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n/an/a 1.70E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50326557
PNG
((E)-5-((2-hydroxynaphthalen-1-yl)diazenyl)naphthal...)
Show SMILES Oc1ccc2ccccc2c1N=Nc1cccc2cc(ccc12)S(O)(=O)=O
Show InChI InChI=1S/C20H14N2O4S/c23-19-11-8-13-4-1-2-6-17(13)20(19)22-21-18-7-3-5-14-12-15(27(24,25)26)9-10-16(14)18/h1-12,23H,(H,24,25,26)
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n/an/a 1.70E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Displacement of 8-NBD-cAMP from EPAC2 (unknown origin) by fluorescence plate reader analysis


J Med Chem 57: 3651-65 (2014)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175143
PNG
(CHEMBL3809313)
Show SMILES Cc1cc(C)c(Nc2c(C)cc(C)cc2C)c(C)c1
Show InChI InChI=1S/C18H23N/c1-11-7-13(3)17(14(4)8-11)19-18-15(5)9-12(2)10-16(18)6/h7-10,19H,1-6H3
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n/an/a 1.70E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of EPAC2 (unknown origin) assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal tru...


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175071
PNG
(CHEMBL3809991)
Show SMILES Cc1cc(C)c(Nc2ccc3CCCc3c2)c(C)c1
Show InChI InChI=1S/C18H21N/c1-12-9-13(2)18(14(3)10-12)19-17-8-7-15-5-4-6-16(15)11-17/h7-11,19H,4-6H2,1-3H3
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n/an/a 1.80E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175264
PNG
(CHEMBL3810082)
Show SMILES Cc1cc(C)c(Nc2ccc(C)c(Cl)c2)c(C)c1
Show InChI InChI=1S/C16H18ClN/c1-10-7-12(3)16(13(4)8-10)18-14-6-5-11(2)15(17)9-14/h5-9,18H,1-4H3
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n/an/a 1.80E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175101
PNG
(CHEMBL3810034)
Show SMILES CCc1cccc(Nc2c(C)cc(C)cc2C)c1
Show InChI InChI=1S/C17H21N/c1-5-15-7-6-8-16(11-15)18-17-13(3)9-12(2)10-14(17)4/h6-11,18H,5H2,1-4H3
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n/an/a 1.80E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175069
PNG
(CHEMBL3808996)
Show SMILES Cc1ccc(C)c(Nc2c(C)cc(C)cc2C)c1
Show InChI InChI=1S/C17H21N/c1-11-6-7-13(3)16(10-11)18-17-14(4)8-12(2)9-15(17)5/h6-10,18H,1-5H3
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n/an/a 1.80E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50425550
PNG
(CHEMBL2313658)
Show SMILES COc1ccc(cc1)S(=O)(=O)c1c(C)cc(C)cc1C
Show InChI InChI=1S/C16H18O3S/c1-11-9-12(2)16(13(3)10-11)20(17,18)15-7-5-14(19-4)6-8-15/h5-10H,1-4H3
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n/an/a 1.90E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay


J Med Chem 56: 952-62 (2013)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175139
PNG
(CHEMBL3810304)
Show SMILES Cc1cc(C)c(Nc2cccc(c2)C(F)(F)F)c(C)c1
Show InChI InChI=1S/C16H16F3N/c1-10-7-11(2)15(12(3)8-10)20-14-6-4-5-13(9-14)16(17,18)19/h4-9,20H,1-3H3
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n/an/a 2.00E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175068
PNG
(CHEMBL3809695)
Show SMILES Cc1ccc(Nc2c(C)cc(C)cc2C)c(C)c1
Show InChI InChI=1S/C17H21N/c1-11-6-7-16(13(3)8-11)18-17-14(4)9-12(2)10-15(17)5/h6-10,18H,1-5H3
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n/an/a 2.20E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50425525
PNG
(CHEMBL2313652)
Show SMILES Cc1cc(C)c(c(C)c1)S(=O)(=O)n1ccc2cccnc12
Show InChI InChI=1S/C16H16N2O2S/c1-11-9-12(2)15(13(3)10-11)21(19,20)18-8-6-14-5-4-7-17-16(14)18/h4-10H,1-3H3
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n/an/a 2.40E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay


J Med Chem 56: 952-62 (2013)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175272
PNG
(CHEMBL3809067)
Show SMILES Cc1cc(C)c(Nc2c(F)cc(F)cc2F)c(C)c1
Show InChI InChI=1S/C15H14F3N/c1-8-4-9(2)14(10(3)5-8)19-15-12(17)6-11(16)7-13(15)18/h4-7,19H,1-3H3
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n/an/a 2.70E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175254
PNG
(CHEMBL3810341)
Show SMILES Cc1cc(C)c(Nc2cc(F)cc(Cl)c2)c(C)c1
Show InChI InChI=1S/C15H15ClFN/c1-9-4-10(2)15(11(3)5-9)18-14-7-12(16)6-13(17)8-14/h4-8,18H,1-3H3
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n/an/a 2.90E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175263
PNG
(CHEMBL3809722)
Show SMILES Cc1cc(C)c(Nc2ccc(F)c(Cl)c2)c(C)c1
Show InChI InChI=1S/C15H15ClFN/c1-9-6-10(2)15(11(3)7-9)18-12-4-5-14(17)13(16)8-12/h4-8,18H,1-3H3
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n/an/a 2.90E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175271
PNG
(CHEMBL3809245)
Show SMILES Cc1cc(C)c(Nc2cc(F)c(F)c(F)c2)c(C)c1
Show InChI InChI=1S/C15H14F3N/c1-8-4-9(2)15(10(3)5-8)19-11-6-12(16)14(18)13(17)7-11/h4-7,19H,1-3H3
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n/an/a 3.00E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175258
PNG
(CHEMBL3810188)
Show SMILES Cc1cc(C)c(Nc2ccc(Cl)c(F)c2)c(C)c1
Show InChI InChI=1S/C15H15ClFN/c1-9-6-10(2)15(11(3)7-9)18-12-4-5-13(16)14(17)8-12/h4-8,18H,1-3H3
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n/an/a 3.30E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50175226
PNG
(CHEMBL3808936)
Show SMILES Cc1cc(C)c(Nc2cccc(Cl)c2C)c(C)c1
Show InChI InChI=1S/C16H18ClN/c1-10-8-11(2)16(12(3)9-10)18-15-7-5-6-14(17)13(15)4/h5-9,18H,1-4H3
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n/an/a 3.60E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of EPAC2 (unknown origin) assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal tru...


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50011357
PNG
(CHEMBL3260988)
Show SMILES OC(O)=C\C=C1/C2=C(Oc3c(O)c(O)ccc13)C(=O)C(=O)C=C2
Show InChI InChI=1S/C16H10O7/c17-10-4-1-8-7(3-6-12(19)20)9-2-5-11(18)14(22)16(9)23-15(8)13(10)21/h1-6,17,19-21H/b7-3-
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n/an/a 3.80E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Displacement of 8-NBD-cAMP from EPAC2 (unknown origin) by fluorescence plate reader analysis


J Med Chem 57: 3651-65 (2014)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50425528
PNG
(CHEMBL2313649)
Show SMILES Cc1cc(C)c(c(C)c1)S(=O)(=O)n1ccc2ncccc12
Show InChI InChI=1S/C16H16N2O2S/c1-11-9-12(2)16(13(3)10-11)21(19,20)18-8-6-14-15(18)5-4-7-17-14/h4-10H,1-3H3
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n/an/a 3.80E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay


J Med Chem 56: 952-62 (2013)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50425543
PNG
(CHEMBL2313635)
Show SMILES Cc1ccc(Nc2c(C)cc(C)cc2C)cc1
Show InChI InChI=1S/C16H19N/c1-11-5-7-15(8-6-11)17-16-13(3)9-12(2)10-14(16)4/h5-10,17H,1-4H3
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n/an/a 3.80E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay


J Med Chem 56: 952-62 (2013)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50384273
PNG
(CHEMBL2030612)
Show SMILES Cc1ccc(C)c(CSc2nc(C3CC3)c(C#N)c(=O)[nH]2)c1
Show InChI InChI=1S/C17H17N3OS/c1-10-3-4-11(2)13(7-10)9-22-17-19-15(12-5-6-12)14(8-18)16(21)20-17/h3-4,7,12H,5-6,9H2,1-2H3,(H,19,20,21)
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n/an/a 4.00E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Competitive inhibition of Epac2 using fluorescent nucleotide analog 8-NBD-cAMP by fluorescence analysis


Bioorg Med Chem Lett 22: 4038-43 (2012)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50425551
PNG
(CHEMBL2313657)
Show SMILES Cc1cc(C)c(c(C)c1)S(=O)(=O)c1ccc(I)cc1
Show InChI InChI=1S/C15H15IO2S/c1-10-8-11(2)15(12(3)9-10)19(17,18)14-6-4-13(16)5-7-14/h4-9H,1-3H3
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n/an/a 4.00E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay


J Med Chem 56: 952-62 (2013)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50425538
PNG
(CHEMBL2313640)
Show SMILES CCc1cccn1S(=O)(=O)c1ccc(C)cc1
Show InChI InChI=1S/C13H15NO2S/c1-3-12-5-4-10-14(12)17(15,16)13-8-6-11(2)7-9-13/h4-10H,3H2,1-2H3
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n/an/a 4.00E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay


J Med Chem 56: 952-62 (2013)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50011360
PNG
(CHEMBL3260990)
Show SMILES CC(C)(C)c1cc(no1)C(=O)C(=N\Nc1cccc(Cl)c1)\C#N
Show InChI InChI=1S/C16H15ClN4O2/c1-16(2,3)14-8-12(21-23-14)15(22)13(9-18)20-19-11-6-4-5-10(17)7-11/h4-8,19H,1-3H3/b20-13+
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n/an/a 4.40E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of recombinant C-terminal FLAG/HA-tagged EPAC2 (unknown origin) expressed in retrovirus infected human HeLaS3 cells assessed as reduction ...


ACS Med Chem Lett 7: 460-4 (2016)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50011360
PNG
(CHEMBL3260990)
Show SMILES CC(C)(C)c1cc(no1)C(=O)C(=N\Nc1cccc(Cl)c1)\C#N
Show InChI InChI=1S/C16H15ClN4O2/c1-16(2,3)14-8-12(21-23-14)15(22)13(9-18)20-19-11-6-4-5-10(17)7-11/h4-8,19H,1-3H3/b20-13+
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Article
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n/an/a 4.40E+3n/an/an/an/an/an/a



?Chemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, Texas 77555, United States.

Curated by ChEMBL


Assay Description
Antagonist activity at EPAC2 (unknown origin) assessed as cAMP-induced guanine nucleotide exchange factor activity


J Med Chem 58: 6033-47 (2015)

More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 4


(Homo sapiens)
BDBM50425533
PNG
(CHEMBL2313644)
Show SMILES CCc1cccn1S(=O)(=O)c1cc(C)cc(C)c1
Show InChI InChI=1S/C14H17NO2S/c1-4-13-6-5-7-15(13)18(16,17)14-9-11(2)8-12(3)10-14/h5-10H,4H2,1-3H3
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Article
PubMed
n/an/a 4.70E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay


J Med Chem 56: 952-62 (2013)

More data for this
Ligand-Target Pair
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