Found 19 hits for monomerid = 50011360 Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kcal/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
Rap guanine nucleotide exchange factor 4
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 7.00E+3 | n/a | n/a | n/a | n/a | n/a | n/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)
Article DOI: 10.1021/jm401425e BindingDB Entry DOI: 10.7270/Q2WH2RJW |
More data for this Ligand-Target Pair | |
Albumin
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB MMDB
NCI pathway Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid UniChem
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Similars
| Article PubMed
| n/a | n/a | n/a | 230 | n/a | n/a | n/a | n/a | n/a |
University Health Network
Curated by ChEMBL
| Assay Description Displacement of dansylated arginine from human serum albumin by fluorescence assay |
J Med Chem 62: 5063-5079 (2019)
Article DOI: 10.1021/acs.jmedchem.9b00258 |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 4
(Mus musculus) | BDBM50011360
(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+ | PDB
UniProtKB/SwissProt UniProtKB/TrEMBL
GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid UniChem
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Similars
| Article PubMed
| n/a | n/a | 8.90E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Texas Medical Branch
Curated by ChEMBL
| Assay Description Displacement of 8-NBD-cAMP from mouse recombinant EPAC2 by fluorescence assay |
J Med Chem 58: 6033-47 (2015)
Article DOI: 10.1021/acs.jmedchem.5b00635 BindingDB Entry DOI: 10.7270/Q29025JD |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 3
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB
KEGG
UniProtKB/SwissProt
GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 1.08E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Texas Medical Branch
Curated by ChEMBL
| Assay Description Antagonist activity at EPAC1 (unknown origin) assessed as cAMP-induced guanine nucleotide exchange factor activity |
J Med Chem 58: 6033-47 (2015)
Article DOI: 10.1021/acs.jmedchem.5b00635 BindingDB Entry DOI: 10.7270/Q29025JD |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 4
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 4.40E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Texas Medical Branch
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)
Article DOI: 10.1021/acs.jmedchem.5b00635 BindingDB Entry DOI: 10.7270/Q29025JD |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 4
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 9.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Texas Medical Branch
Curated by ChEMBL
| Assay Description Displacement of 8-NBD-cAMP from EPAC2 (unknown origin) |
J Med Chem 58: 6033-47 (2015)
Article DOI: 10.1021/acs.jmedchem.5b00635 BindingDB Entry DOI: 10.7270/Q29025JD |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 3
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB
KEGG
UniProtKB/SwissProt
GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 1.08E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Texas Medical Branch
Curated by ChEMBL
| Assay Description Antagonist activity at human recombinant EPAC1 assessed as inhibition of Rap1b-bGDP exchange activity |
J Med Chem 58: 6033-47 (2015)
Article DOI: 10.1021/acs.jmedchem.5b00635 BindingDB Entry DOI: 10.7270/Q29025JD |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 3
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB
KEGG
UniProtKB/SwissProt
GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| PubMed
| n/a | n/a | 1.08E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Texas Medical Branch
Curated by ChEMBL
| Assay Description Inhibition of recombinant C-terminal FLAG/HA-tagged EPAC1 (unknown origin) expressed in retrovirus infected human HeLaS3 cells assessed as reduction ... |
ACS Med Chem Lett 7: 460-4 (2016)
BindingDB Entry DOI: 10.7270/Q2NC6335 |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 4
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| PubMed
| n/a | n/a | 4.40E+3 | n/a | n/a | n/a | n/a | n/a | n/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)
BindingDB Entry DOI: 10.7270/Q2NC6335 |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 3
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB
KEGG
UniProtKB/SwissProt
GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 1.08E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Texas Medical Branch
Curated by ChEMBL
| Assay Description Antagonist activity at recombinant human full length EPAC1 assessed as inhibition of EPAC1-mediated Rap1B (1 to 167 residues)-BODIPY GDP nucleotide e... |
Eur J Med Chem 134: 62-71 (2017)
Article DOI: 10.1016/j.ejmech.2017.04.001 BindingDB Entry DOI: 10.7270/Q2RR21DK |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 4
(Mus musculus) | BDBM50011360
(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+ | PDB
UniProtKB/SwissProt UniProtKB/TrEMBL
GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 4.40E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Texas Medical Branch
Curated by ChEMBL
| Assay Description In vito concentration required to displace [3H]cyclofoxy (Kd = 0.8 nM and concentration is 1.3 nM) from mu and kappa2 receptor in rat brain membranes... |
Eur J Med Chem 134: 62-71 (2017)
Article DOI: 10.1016/j.ejmech.2017.04.001 BindingDB Entry DOI: 10.7270/Q2RR21DK |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 3
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB
KEGG
UniProtKB/SwissProt
GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 9.10E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Texas Medical Branch
Curated by ChEMBL
| Assay Description Antagonist activity at recombinant full length EPAC1 (unknown origin) assessed as inhibition of cAMP-mediated Rap1b-BODIPY GDP nucleotide exchange ac... |
Bioorg Med Chem Lett 27: 5163-5166 (2017)
Article DOI: 10.1016/j.bmcl.2017.10.056 BindingDB Entry DOI: 10.7270/Q2TB19FF |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 4
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 4.40E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Texas Medical Branch
Curated by ChEMBL
| Assay Description Antagonist activity at recombinant full length EPAC2 (unknown origin) assessed as inhibition of cAMP-mediated Rap1b-BODIPY GDP nucleotide exchange ac... |
Bioorg Med Chem Lett 27: 5163-5166 (2017)
Article DOI: 10.1016/j.bmcl.2017.10.056 BindingDB Entry DOI: 10.7270/Q2TB19FF |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 3
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB
KEGG
UniProtKB/SwissProt
GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 3.20E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Texas Medical Branch
Curated by ChEMBL
| Assay Description Inhibition of EPAC1 (unknown origin) |
Bioorg Med Chem Lett 27: 1633-1639 (2017)
Article DOI: 10.1016/j.bmcl.2017.02.065 BindingDB Entry DOI: 10.7270/Q2FF3VXQ |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 4
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 7.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Texas Medical Branch
Curated by ChEMBL
| Assay Description Inhibition of EPAC2 (unknown origin) |
Bioorg Med Chem Lett 27: 1633-1639 (2017)
Article DOI: 10.1016/j.bmcl.2017.02.065 BindingDB Entry DOI: 10.7270/Q2FF3VXQ |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 3
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB
KEGG
UniProtKB/SwissProt
GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | n/a | 2.00E+4 | n/a | n/a | n/a | n/a | n/a |
University Health Network
Curated by ChEMBL
| Assay Description Inhibition of 8-NBD-cAMP binding to human EPAC1 cAMP binding domain (149 to 318 residues) by fluorescence assay |
J Med Chem 62: 5063-5079 (2019)
Article DOI: 10.1021/acs.jmedchem.9b00258 |
More data for this Ligand-Target Pair | |
Albumin
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB MMDB
NCI pathway Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | n/a | 99 | n/a | n/a | n/a | n/a | n/a |
University Health Network
Curated by ChEMBL
| Assay Description Displacement of dansylated phenylalanine from human serum albumin by fluorescence assay |
J Med Chem 62: 5063-5079 (2019)
Article DOI: 10.1021/acs.jmedchem.9b00258 |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 3
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB
KEGG
UniProtKB/SwissProt
GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | n/a | 2.00E+4 | n/a | n/a | n/a | n/a | n/a |
University Health Network
Curated by ChEMBL
| Assay Description Binding affinity to human EPAC1 cAMP binding domain (149 to 318 residues) using aggregate form of compound by [15N-1H]HSQC spectroscopic analysis |
J Med Chem 62: 5063-5079 (2019)
Article DOI: 10.1021/acs.jmedchem.9b00258 |
More data for this Ligand-Target Pair | |
Rap guanine nucleotide exchange factor 3
(Homo sapiens (Human)) | BDBM50011360
(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+ | PDB
KEGG
UniProtKB/SwissProt
GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 3.20E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Texas Medical Branch
Curated by ChEMBL
| Assay Description Inhibition of EPAC1 (unknown origin) assessed as cAMP-mediated GEF activity |
J Med Chem 57: 3651-65 (2014)
Article DOI: 10.1021/jm401425e BindingDB Entry DOI: 10.7270/Q2WH2RJW |
More data for this Ligand-Target Pair | |