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Found 15 hits Enz. Inhib. hit(s) with Target = 'Rap guanine nucleotide exchange factor 3' 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 3


(Homo sapiens)
BDBM50098719
PNG
(CHEMBL3593329)
Show SMILES CC(C)(C)c1cc(no1)C(=O)C(=N\Nc1cc(Cl)cc(Cl)c1)\C#N
Show InChI InChI=1S/C16H14Cl2N4O2/c1-16(2,3)14-7-12(22-24-14)15(23)13(8-19)21-20-11-5-9(17)4-10(18)6-11/h4-7,20H,1-3H3/b21-13+
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PubMed
n/an/a 2.40E+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 human recombinant EPAC1 assessed as inhibition of Rap1b-bGDP exchange activity


Citation and Details
More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 3


(Homo sapiens)
BDBM50098793
PNG
(CHEMBL3593342)
Show SMILES CC(C)(C)c1cc(no1)C(=O)C(=N\Nc1cc(Cl)c(Cl)c(Cl)c1)\C#N
Show InChI InChI=1S/C16H13Cl3N4O2/c1-16(2,3)13-6-11(23-25-13)15(24)12(7-20)22-21-8-4-9(17)14(19)10(18)5-8/h4-6,21H,1-3H3/b22-12+
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n/an/a 2.40E+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 human recombinant EPAC1 assessed as inhibition of Rap1b-bGDP exchange activity


Citation and Details
More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 3


(Homo sapiens)
BDBM50098787
PNG
(CHEMBL3593468)
Show SMILES Clc1cc(Cl)cc(N\N=C(/C#N)C(=O)c2cc(on2)C2CCCCC2)c1
Show InChI InChI=1S/C18H16Cl2N4O2/c19-12-6-13(20)8-14(7-12)22-23-16(10-21)18(25)15-9-17(26-24-15)11-4-2-1-3-5-11/h6-9,11,22H,1-5H2/b23-16+
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n/an/a 2.60E+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 human recombinant EPAC1 assessed as inhibition of Rap1b-bGDP exchange activity


Citation and Details
More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 3


(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 3.20E+3n/an/an/an/an/an/a



University of Texas Medical Branch

Curated by ChEMBL


Assay Description
Inhibition of EPAC1 (unknown origin) assessed as cAMP-mediated GEF activity


Citation and Details
More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 3


(Homo sapiens)
BDBM50098797
PNG
(CHEMBL3593471)
Show SMILES Clc1cc(N\N=C(/C#N)C(=O)c2cc(on2)C2CCCCC2)cc(Cl)c1Cl
Show InChI InChI=1S/C18H15Cl3N4O2/c19-12-6-11(7-13(20)17(12)21)23-24-15(9-22)18(26)14-8-16(27-25-14)10-4-2-1-3-5-10/h6-8,10,23H,1-5H2/b24-15+
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n/an/a 4.00E+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 human recombinant EPAC1 assessed as inhibition of Rap1b-bGDP exchange activity


Citation and Details
More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 3


(Homo sapiens)
BDBM50098796
PNG
(CHEMBL3593470)
Show SMILES Clc1cc(N\N=C(/C#N)C(=O)c2cc(on2)C2CC2)cc(Cl)c1Cl
Show InChI InChI=1S/C15H9Cl3N4O2/c16-9-3-8(4-10(17)14(9)18)20-21-12(6-19)15(23)11-5-13(24-22-11)7-1-2-7/h3-5,7,20H,1-2H2/b21-12+
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n/an/a 4.10E+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 human recombinant EPAC1 assessed as inhibition of Rap1b-bGDP exchange activity


Citation and Details
More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 3


(Homo sapiens)
BDBM50098794
PNG
(CHEMBL3593341)
Show SMILES CC(C)(C)c1cc(no1)C(=O)C(=N\Nc1ccc(c(Cl)c1)C(F)(F)F)\C#N
Show InChI InChI=1S/C17H14ClF3N4O2/c1-16(2,3)14-7-12(25-27-14)15(26)13(8-22)24-23-9-4-5-10(11(18)6-9)17(19,20)21/h4-7,23H,1-3H3/b24-13+
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PubMed
n/an/a 4.30E+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 human recombinant EPAC1 assessed as inhibition of Rap1b-bGDP exchange activity


Citation and Details
More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 3


(Homo sapiens)
BDBM50098713
PNG
(CHEMBL3593335)
Show SMILES CC(C)(C)c1cc(no1)C(=O)C(=N\Nc1cc(Cl)cc(c1)C(F)(F)F)\C#N
Show InChI InChI=1S/C17H14ClF3N4O2/c1-16(2,3)14-7-12(25-27-14)15(26)13(8-22)24-23-11-5-9(17(19,20)21)4-10(18)6-11/h4-7,23H,1-3H3/b24-13+
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n/an/a 5.70E+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 human recombinant EPAC1 assessed as inhibition of Rap1b-bGDP exchange activity


Citation and Details
More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 3


(Homo sapiens)
BDBM50098716
PNG
(CHEMBL3593332)
Show SMILES CC(C)(C)c1cc(no1)C(=O)C(=N\Nc1cc(cc(c1)C(F)(F)F)C(F)(F)F)\C#N
Show InChI InChI=1S/C18H14F6N4O2/c1-16(2,3)14-7-12(28-30-14)15(29)13(8-25)27-26-11-5-9(17(19,20)21)4-10(6-11)18(22,23)24/h4-7,26H,1-3H3/b27-13+
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n/an/a 5.70E+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 human recombinant EPAC1 assessed as inhibition of Rap1b-bGDP exchange activity


Citation and Details
More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 3


(Homo sapiens)
BDBM50098709
PNG
(CHEMBL3593338)
Show SMILES CC(C)(C)c1cc(no1)C(=O)C(=N\Nc1ccc(F)c(Cl)c1)\C#N
Show InChI InChI=1S/C16H14ClFN4O2/c1-16(2,3)14-7-12(22-24-14)15(23)13(8-19)21-20-9-4-5-11(18)10(17)6-9/h4-7,20H,1-3H3/b21-13+
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n/an/a 7.80E+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 human recombinant EPAC1 assessed as inhibition of Rap1b-bGDP exchange activity


Citation and Details
More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 3


(Homo sapiens)
BDBM50098792
PNG
(CHEMBL3593343)
Show SMILES CC(C)(C)c1cc(no1)C(=O)C(=N\Nc1cc(F)c(F)c(F)c1)\C#N
Show InChI InChI=1S/C16H13F3N4O2/c1-16(2,3)13-6-11(23-25-13)15(24)12(7-20)22-21-8-4-9(17)14(19)10(18)5-8/h4-6,21H,1-3H3/b22-12+
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n/an/a 8.90E+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 human recombinant EPAC1 assessed as inhibition of Rap1b-bGDP exchange activity


Citation and Details
More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 3


(Homo sapiens)
BDBM50098748
PNG
(CHEMBL3593339)
Show SMILES CC(C)(C)c1cc(no1)C(=O)C(=N\Nc1ccc(Cl)c(c1)C(F)(F)F)\C#N
Show InChI InChI=1S/C12H20N4O7/c1-4(18)15-8-5(16-12(13)14)2-7(11(21)22)23-10(8)9(20)6(19)3-17/h2,5-6,8-10,17,19-20H,3H2,1H3,(H,15,18)(H,21,22)(H4,13,14,16)/t5-,6-,8+,9?,10?/m0/s1
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n/an/a 9.70E+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 human recombinant EPAC1 assessed as inhibition of Rap1b-bGDP exchange activity


Citation and Details
More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 3


(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 1.08E+4n/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 human recombinant EPAC1 assessed as inhibition of Rap1b-bGDP exchange activity


Citation and Details
More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 3


(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 1.08E+4n/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 EPAC1 (unknown origin) assessed as cAMP-induced guanine nucleotide exchange factor activity


Citation and Details
More data for this
Ligand-Target Pair
Rap guanine nucleotide exchange factor 3


(Homo sapiens)
BDBM50098712
PNG
(CHEMBL3593336)
Show SMILES CC(C)(C)c1cc(no1)C(=O)C(=N\Nc1cc(F)cc(Cl)c1)\C#N
Show InChI InChI=1S/C16H14ClFN4O2/c1-16(2,3)14-7-12(22-24-14)15(23)13(8-19)21-20-11-5-9(17)4-10(18)6-11/h4-7,20H,1-3H3/b21-13+
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n/an/a 1.16E+4n/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 human recombinant EPAC1 assessed as inhibition of Rap1b-bGDP exchange activity


Citation and Details
More data for this
Ligand-Target Pair