Found 17 hits of ic50 for UniProtKB: P78362 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 |
|---|
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM50500357
(CHEMBL3746522 | US11066363, Compound 31)Show SMILES CCc1cc2C(=O)c3c([nH]c4cc(ccc34)C#N)C(C)(C)c2cc1-c1cnn(CCN(C)C)c1 Show InChI InChI=1S/C28H29N5O/c1-6-18-12-22-23(13-21(18)19-15-30-33(16-19)10-9-32(4)5)28(2,3)27-25(26(22)34)20-8-7-17(14-29)11-24(20)31-27/h7-8,11-13,15-16,31H,6,9-10H2,1-5H3 | PDB
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| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 6.60 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
SRPK1 Inhibitory Activities of the Compounds. |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2P55RN2 |
More data for this
Ligand-Target Pair | |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM50500359
(CHEMBL3747611 | US11066363, Compound 13)Show SMILES CCc1cc2C(=O)c3c([nH]c4cc(ccc34)C#N)C(C)(C)c2cc1-c1cnn[nH]1 Show InChI InChI=1S/C23H19N5O/c1-4-13-8-16-17(9-15(13)19-11-25-28-27-19)23(2,3)22-20(21(16)29)14-6-5-12(10-24)7-18(14)26-22/h5-9,11,26H,4H2,1-3H3,(H,25,27,28) | PDB
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| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 7.46 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
SRPK1 Inhibitory Activities of the Compounds. |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2P55RN2 |
More data for this
Ligand-Target Pair | |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM50500351
(CHEMBL3746960 | US11066363, Compound 19)Show SMILES CCc1cc2C(=O)c3c([nH]c4cc(ccc34)C#N)C(C)(C)c2cc1N1CCN(C)CC1 Show InChI InChI=1S/C26H28N4O/c1-5-17-13-19-20(14-22(17)30-10-8-29(4)9-11-30)26(2,3)25-23(24(19)31)18-7-6-16(15-27)12-21(18)28-25/h6-7,12-14,28H,5,8-11H2,1-4H3 | PDB
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| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 8.57 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
SRPK1 Inhibitory Activities of the Compounds. |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2P55RN2 |
More data for this
Ligand-Target Pair | |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM50500356
(CHEMBL3747406 | US11066363, Compound 7)Show SMILES CCc1cc2C(=O)c3c([nH]c4cc(ccc34)C#N)C(C)(C)c2cc1-c1cnn(C)c1 Show InChI InChI=1S/C25H22N4O/c1-5-15-9-19-20(10-18(15)16-12-27-29(4)13-16)25(2,3)24-22(23(19)30)17-7-6-14(11-26)8-21(17)28-24/h6-10,12-13,28H,5H2,1-4H3 | PDB
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| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 12.4 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
SRPK1 Inhibitory Activities of the Compounds. |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2P55RN2 |
More data for this
Ligand-Target Pair | |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM504520
(9-ethyl-6,6-dimethyl-11-oxo-8- (pyrimidin-5-yl)-6,...)Show SMILES CCc1cc2C(=O)c3c([nH]c4cc(ccc34)C#N)C(C)(C)c2cc1-c1cncnc1 | PDB
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| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 12.5 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
SRPK1 Inhibitory Activities of the Compounds. |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2P55RN2 |
More data for this
Ligand-Target Pair | |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM504519
((9-ethyl-6,6-dimethyl-11-oxo-8- (pyridin-4-yl)-6,1...)Show SMILES CCc1cc2C(=O)c3c([nH]c4cc(ccc34)C#N)C(C)(C)c2cc1-c1ccncc1 | PDB
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| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 13.2 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
SRPK1 Inhibitory Activities of the Compounds. |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2P55RN2 |
More data for this
Ligand-Target Pair | |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM50500353
(CHEMBL3746395 | US11066363, Compound 10)Show SMILES CCc1cc2C(=O)c3c([nH]c4cc(ccc34)C#N)C(C)(C)c2cc1-c1cnoc1 Show InChI InChI=1S/C24H19N3O2/c1-4-14-8-18-19(9-17(14)15-11-26-29-12-15)24(2,3)23-21(22(18)28)16-6-5-13(10-25)7-20(16)27-23/h5-9,11-12,27H,4H2,1-3H3 | PDB
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| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 14.5 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
SRPK1 Inhibitory Activities of the Compounds. |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2P55RN2 |
More data for this
Ligand-Target Pair | |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM50500355
(CHEMBL3747108 | US11066363, Compound 36)Show SMILES CCc1cc2C(=O)c3c([nH]c4cc(ccc34)C#N)C(C)(C)c2cc1-c1cnn(c1)C(=O)N(C)C Show InChI InChI=1S/C27H25N5O2/c1-6-16-10-20-21(11-19(16)17-13-29-32(14-17)26(34)31(4)5)27(2,3)25-23(24(20)33)18-8-7-15(12-28)9-22(18)30-25/h7-11,13-14,30H,6H2,1-5H3 | PDB
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| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 23.6 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
SRPK1 Inhibitory Activities of the Compounds. |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2P55RN2 |
More data for this
Ligand-Target Pair | |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM50362781
(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)Show SMILES CCc1cc2C(=O)c3c([nH]c4cc(ccc34)C#N)C(C)(C)c2cc1N1CCC(CC1)N1CCOCC1 Show InChI InChI=1S/C30H34N4O2/c1-4-20-16-23-24(17-26(20)34-9-7-21(8-10-34)33-11-13-36-14-12-33)30(2,3)29-27(28(23)35)22-6-5-19(18-31)15-25(22)32-29/h5-6,15-17,21,32H,4,7-14H2,1-3H3 | PDB
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| US Patent
| n/a | n/a | 28.2 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
SRPK1 Inhibitory Activities of the Compounds. |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2P55RN2 |
More data for this
Ligand-Target Pair | |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM50512854
(CHEMBL4468747 | US11066363, Compound 37)Show SMILES CCc1cc2C(=O)c3c([nH]c4cc(ccc34)C#N)C(C)(C)c2cc1-c1cccc(c1)S(F)(=O)=O Show InChI InChI=1S/C27H21FN2O3S/c1-4-16-12-21-22(13-20(16)17-6-5-7-18(11-17)34(28,32)33)27(2,3)26-24(25(21)31)19-9-8-15(14-29)10-23(19)30-26/h5-13,30H,4H2,1-3H3 | PDB
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| Article
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| n/a | n/a | 98 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
Article DOI: 10.1016/j.bmc.2022.116921
BindingDB Entry DOI: 10.7270/Q25B06FX |
More data for this
Ligand-Target Pair | |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM2579
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r| Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1 | PDB
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| Article
PubMed
| n/a | n/a | 185 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of human SRPK2 using GRSRSRSRSR as substrate by [gamma-33P]-ATP assay |
Citation and Details
Article DOI: 10.1016/j.bmc.2018.02.022
BindingDB Entry DOI: 10.7270/Q2DJ5KB8 |
More data for this
Ligand-Target Pair | |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM50564378
(CHEMBL4787157)Show SMILES COc1cc(\C=C2\C(=N)N3N=C(SC3=NC2=O)C(F)(F)F)ccc1O |c:10,14| | PDB
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| n/a | n/a | 203 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
Article DOI: 10.1016/j.bmc.2022.116921
BindingDB Entry DOI: 10.7270/Q25B06FX |
More data for this
Ligand-Target Pair | |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM2579
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r| Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1 | PDB
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| Article
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| n/a | n/a | 227 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Florida
Curated by ChEMBL
| Assay Description
Inhibition of human SRPK2 using GRSRSRSRSR as substrate by [gamma-33P]-ATP assay |
Eur J Med Chem 161: 456-467 (2019)
Article DOI: 10.1016/j.ejmech.2018.10.052
BindingDB Entry DOI: 10.7270/Q2W380MT |
More data for this
Ligand-Target Pair | |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM50235034
(CHEMBL4064277)Show InChI InChI=1S/C18H18F3N3O/c19-18(20,21)14-4-5-16(24-10-2-1-3-11-24)15(12-14)23-17(25)13-6-8-22-9-7-13/h4-9,12H,1-3,10-11H2,(H,23,25) | PDB
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| PDB
Article
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| n/a | n/a | 7.40E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
Article DOI: 10.1016/j.bmc.2022.116921
BindingDB Entry DOI: 10.7270/Q25B06FX |
More data for this
Ligand-Target Pair | 
3D Structure (crystal) |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM50519662
(CHEMBL4438748)Show SMILES CN(C)c1ccc(cc1)C(=O)Nc1cccc(NC(=O)COc2ccc3c(c2)occc3=O)c1 Show InChI InChI=1S/C26H23N3O5/c1-29(2)20-8-6-17(7-9-20)26(32)28-19-5-3-4-18(14-19)27-25(31)16-34-21-10-11-22-23(30)12-13-33-24(22)15-21/h3-15H,16H2,1-2H3,(H,27,31)(H,28,32) | PDB
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| n/a | n/a | >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description
Inhibition of recombinant human SRPK2 (46 to end residues) using RSRSRSRSRSRSRSR as substrate incubated for 40 mins in presence of [gamma33P]ATP by r... |
J Med Chem 62: 10691-10710 (2019)
Article DOI: 10.1021/acs.jmedchem.9b01143
BindingDB Entry DOI: 10.7270/Q2MC93FG |
More data for this
Ligand-Target Pair | |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM50135286
(CHEMBL3745885)Show SMILES Cn1c2nc(Nc3ccc4[nH]ccc4c3)ncc2cc(c1=O)S(=O)(=O)c1ccc(F)cc1F Show InChI InChI=1S/C22H15F2N5O3S/c1-29-20-13(9-19(21(29)30)33(31,32)18-5-2-14(23)10-16(18)24)11-26-22(28-20)27-15-3-4-17-12(8-15)6-7-25-17/h2-11,25H,1H3,(H,26,27,28) | PDB
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| n/a | n/a | >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Icahn School of Medicine at Mount Sinai
Curated by ChEMBL
| Assay Description
Inhibition of human SRPK2 using [GRSRSRSRSR] as substrate |
Bioorg Med Chem 24: 521-44 (2016)
Article DOI: 10.1016/j.bmc.2015.11.045
BindingDB Entry DOI: 10.7270/Q24Q7WT8 |
More data for this
Ligand-Target Pair | |
SRSF protein kinase 2
(Homo sapiens (Human)) | BDBM50537742
(CHEMBL4634634 | US11179389, Compound 1-14)Show SMILES C[C@@H]1C[C@H]1C(=O)N1CCN(C[C@H]1C)c1cnc(C#N)c(n1)-c1cnn(C)c1 |r| Show InChI InChI=1S/C19H23N7O/c1-12-6-15(12)19(27)26-5-4-25(10-13(26)2)17-9-21-16(7-20)18(23-17)14-8-22-24(3)11-14/h8-9,11-13,15H,4-6,10H2,1-3H3/t12-,13-,15-/m1/s1 | PDB
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| n/a | n/a | >1.00E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
Merck & Co.
Curated by ChEMBL
| Assay Description
Inhibition of recombinant full length human GST-tagged SRPK2 expressed in baculovirus expression system using serine/threonine-07 peptide as substrat... |
Bioorg Med Chem Lett 30: (2020)
Article DOI: 10.1016/j.bmcl.2019.126715
BindingDB Entry DOI: 10.7270/Q2HM5CZG |
More data for this
Ligand-Target Pair | |
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