Found 12 hits Enz. Inhib. hit(s) with Target = 'Transient receptor potential cation channel subfamily V member 4' and Ligand = 'BDBM50192821' Target/Host (Institution) | Ligand | Target/Host 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 | pH | Temp °C |
Transient receptor potential cation channel subfamily V member 4
(Mus musculus) | BDBM50192821
(CHEMBL2133556)Show SMILES Cc1c(cc(-c2ccccc2)n1CCCN1CCOCC1)C(=O)Nc1cccc(c1)C(F)(F)F Show InChI InChI=1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
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| PDB Article PubMed
| n/a | n/a | 17 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description Antagonist activity at mouse TRPV4 |
Citation and Details
Article DOI: 10.1016/j.bmc.2020.115609 BindingDB Entry DOI: 10.7270/Q2RB789W |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 4
(Mus musculus) | BDBM50192821
(CHEMBL2133556)Show SMILES Cc1c(cc(-c2ccccc2)n1CCCN1CCOCC1)C(=O)Nc1cccc(c1)C(F)(F)F Show InChI InChI=1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
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| PDB Article PubMed
| n/a | n/a | 17 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description Antagonist activity at mouse TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced current at holding potential of -40 mV by W... |
ACS Med Chem Lett 8: 549-554 (2017)
Article DOI: 10.1021/acsmedchemlett.7b00094 BindingDB Entry DOI: 10.7270/Q2HD7XWW |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 4
(Homo sapiens (Human)) | BDBM50192821
(CHEMBL2133556)Show SMILES Cc1c(cc(-c2ccccc2)n1CCCN1CCOCC1)C(=O)Nc1cccc(c1)C(F)(F)F Show InChI InChI=1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33) | PDB
UniProtKB/SwissProt
antibodypedia GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid PDB UniChem
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| PDB Article PubMed
| n/a | n/a | 18 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description Antagonist activity at human TRPV4 |
Citation and Details
Article DOI: 10.1016/j.bmc.2020.115609 BindingDB Entry DOI: 10.7270/Q2RB789W |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 4
(Homo sapiens (Human)) | BDBM50192821
(CHEMBL2133556)Show SMILES Cc1c(cc(-c2ccccc2)n1CCCN1CCOCC1)C(=O)Nc1cccc(c1)C(F)(F)F Show InChI InChI=1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33) | PDB
UniProtKB/SwissProt
antibodypedia GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid PDB UniChem
Similars
| PDB Article PubMed
| n/a | n/a | 29 | n/a | n/a | n/a | n/a | n/a | n/a |
Shionogi& Co., Ltd
Curated by ChEMBL
| Assay Description Antagonist activity at recombinant human TRPV4 expressed in CHOK1 cells assessed as inhibition of hypotonicity-induced activation pretreated for 5 mi... |
Bioorg Med Chem 25: 2177-2190 (2017)
Article DOI: 10.1016/j.bmc.2017.02.047 BindingDB Entry DOI: 10.7270/Q2N58PT9 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 4
(Homo sapiens (Human)) | BDBM50192821
(CHEMBL2133556)Show SMILES Cc1c(cc(-c2ccccc2)n1CCCN1CCOCC1)C(=O)Nc1cccc(c1)C(F)(F)F Show InChI InChI=1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33) | PDB
UniProtKB/SwissProt
antibodypedia GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid PDB UniChem
Similars
| PDB Article PubMed
| n/a | n/a | 48 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description Antagonist activity at TRPV4 (unknown origin) |
Bioorg Med Chem Lett 30: (2020)
Article DOI: 10.1016/j.bmcl.2020.127022 BindingDB Entry DOI: 10.7270/Q29G5RC5 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 4
(Homo sapiens (Human)) | BDBM50192821
(CHEMBL2133556)Show SMILES Cc1c(cc(-c2ccccc2)n1CCCN1CCOCC1)C(=O)Nc1cccc(c1)C(F)(F)F Show InChI InChI=1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33) | PDB
UniProtKB/SwissProt
antibodypedia GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid PDB UniChem
Similars
| PDB Article PubMed
| n/a | n/a | 48 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description Antagonist activity at human TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced current at holding potential of -40 mV by W... |
ACS Med Chem Lett 8: 549-554 (2017)
Article DOI: 10.1021/acsmedchemlett.7b00094 BindingDB Entry DOI: 10.7270/Q2HD7XWW |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 4
(Homo sapiens (Human)) | BDBM50192821
(CHEMBL2133556)Show SMILES Cc1c(cc(-c2ccccc2)n1CCCN1CCOCC1)C(=O)Nc1cccc(c1)C(F)(F)F Show InChI InChI=1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33) | PDB
UniProtKB/SwissProt
antibodypedia GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid PDB UniChem
Similars
| PDB Article PubMed
| n/a | n/a | 57 | n/a | n/a | n/a | n/a | n/a | n/a |
Shionogi& Co., Ltd
Curated by ChEMBL
| Assay Description Antagonist activity at recombinant human TRPV4 expressed in CHOK1 cells assessed as inhibition of 4alphaPDD-induced activation pretreated for 5 mins ... |
Bioorg Med Chem 25: 2177-2190 (2017)
Article DOI: 10.1016/j.bmc.2017.02.047 BindingDB Entry DOI: 10.7270/Q2N58PT9 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 4
(Homo sapiens (Human)) | BDBM50192821
(CHEMBL2133556)Show SMILES Cc1c(cc(-c2ccccc2)n1CCCN1CCOCC1)C(=O)Nc1cccc(c1)C(F)(F)F Show InChI InChI=1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33) | PDB
UniProtKB/SwissProt
antibodypedia GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid PDB UniChem
Similars
| PDB Article PubMed
| n/a | n/a | 57 | n/a | n/a | n/a | n/a | n/a | n/a |
Shionogi& Co., Ltd
Curated by ChEMBL
| Assay Description Antagonist activity at human TRPV4 assessed as inhibition of 4alpha-PDD-induced activation |
Bioorg Med Chem Lett 26: 4936-4941 (2016)
Article DOI: 10.1016/j.bmcl.2016.09.014 BindingDB Entry DOI: 10.7270/Q2154K06 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 4
(Homo sapiens (Human)) | BDBM50192821
(CHEMBL2133556)Show SMILES Cc1c(cc(-c2ccccc2)n1CCCN1CCOCC1)C(=O)Nc1cccc(c1)C(F)(F)F Show InChI InChI=1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33) | PDB
UniProtKB/SwissProt
antibodypedia GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid PDB UniChem
Similars
| PDB Article PubMed
| n/a | n/a | 57 | n/a | n/a | n/a | n/a | n/a | n/a |
Shionogi& Co., Ltd.
Curated by ChEMBL
| Assay Description Antagonist activity at human recombinant TRPV4 expressed in CHO-K1 cells assessed as blockade of 1000 nM 4alphaPDD-induced calcium mobilization by FL... |
Bioorg Med Chem Lett 26: 4930-4935 (2016)
Article DOI: 10.1016/j.bmcl.2016.09.013 BindingDB Entry DOI: 10.7270/Q2BC41H5 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 4
(Rattus norvegicus) | BDBM50192821
(CHEMBL2133556)Show SMILES Cc1c(cc(-c2ccccc2)n1CCCN1CCOCC1)C(=O)Nc1cccc(c1)C(F)(F)F Show InChI InChI=1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid PDB UniChem
Similars
| PDB Article PubMed
| n/a | n/a | 133 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description Antagonist activity at rat TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced current at holding potential of -40 mV by Who... |
ACS Med Chem Lett 8: 549-554 (2017)
Article DOI: 10.1021/acsmedchemlett.7b00094 BindingDB Entry DOI: 10.7270/Q2HD7XWW |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 4
(Rattus norvegicus) | BDBM50192821
(CHEMBL2133556)Show SMILES Cc1c(cc(-c2ccccc2)n1CCCN1CCOCC1)C(=O)Nc1cccc(c1)C(F)(F)F Show InChI InChI=1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid PDB UniChem
Similars
| PDB Article PubMed
| n/a | n/a | 133 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description Antagonist activity at rat TRPV4 |
Citation and Details
Article DOI: 10.1016/j.bmc.2020.115609 BindingDB Entry DOI: 10.7270/Q2RB789W |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 4
(Rattus norvegicus) | BDBM50192821
(CHEMBL2133556)Show SMILES Cc1c(cc(-c2ccccc2)n1CCCN1CCOCC1)C(=O)Nc1cccc(c1)C(F)(F)F Show InChI InChI=1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid PDB UniChem
Similars
| PDB Article PubMed
| n/a | n/a | 180 | n/a | n/a | n/a | n/a | n/a | n/a |
Shionogi& Co., Ltd
Curated by ChEMBL
| Assay Description Antagonist activity at recombinant rat TRPV4 expressed in CHOK1 cells assessed as inhibition of 4alphaPDD-induced activation pretreated for 5 mins fo... |
Bioorg Med Chem 25: 2177-2190 (2017)
Article DOI: 10.1016/j.bmc.2017.02.047 BindingDB Entry DOI: 10.7270/Q2N58PT9 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |