Found 13 hits of ki for UniProtKB: P06213 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 |
|---|
Insulin receptor
(Homo sapiens (Human)) | BDBM50256480
(CHEMBL466397 | N-(2,6-difluorophenyl)-5-(3-(2-(5-e...)Show SMILES CCc1cc(Nc2nccc(n2)-c2c(nc3ccccn23)-c2ccc(OC)c(c2)C(=O)Nc2c(F)cccc2F)c(OC)cc1N1CCC(CC1)N1CCN(CC1)S(C)(=O)=O Show InChI InChI=1S/C44H47F2N9O5S/c1-5-28-26-35(38(60-3)27-36(28)53-19-15-30(16-20-53)52-21-23-54(24-22-52)61(4,57)58)49-44-47-17-14-34(48-44)42-40(50-39-11-6-7-18-55(39)42)29-12-13-37(59-2)31(25-29)43(56)51-41-32(45)9-8-10-33(41)46/h6-14,17-18,25-27,30H,5,15-16,19-24H2,1-4H3,(H,51,56)(H,47,48,49) | PDB
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| 1.30 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description
Binding affinity to insulin receptor by liquid scintillation counting |
Bioorg Med Chem Lett 19: 1004-8 (2009)
Article DOI: 10.1016/j.bmcl.2008.11.058
BindingDB Entry DOI: 10.7270/Q24T6J8M |
More data for this
Ligand-Target Pair | |
Insulin receptor
(Homo sapiens (Human)) | BDBM50256478
(CHEMBL507714 | N-(2,6-difluorophenyl)-3-(3-(2-(2-m...)Show SMILES COc1cc(ccc1Nc1nccc(n1)-c1c(nc2ccccn12)-c1cccc(c1)C(=O)Nc1c(F)cccc1F)N1CCC(CC1)N1CCN(CC1)S(C)(=O)=O Show InChI InChI=1S/C41H41F2N9O4S/c1-56-35-26-30(49-19-15-29(16-20-49)50-21-23-51(24-22-50)57(2,54)55)12-13-33(35)45-41-44-17-14-34(46-41)39-37(47-36-11-3-4-18-52(36)39)27-7-5-8-28(25-27)40(53)48-38-31(42)9-6-10-32(38)43/h3-14,17-18,25-26,29H,15-16,19-24H2,1-2H3,(H,48,53)(H,44,45,46) | PDB
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| 2.20 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description
Binding affinity to insulin receptor by liquid scintillation counting |
Bioorg Med Chem Lett 19: 1004-8 (2009)
Article DOI: 10.1016/j.bmcl.2008.11.058
BindingDB Entry DOI: 10.7270/Q24T6J8M |
More data for this
Ligand-Target Pair | |
Insulin receptor
(Homo sapiens (Human)) | BDBM50341519
((S)-3-(4-(2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl...)Show SMILES CNc1cncc(n1)-c1c[nH]c(=O)c(NC(=O)c2ccc(cc2)N2CCC[C@H]2CN2CCCC2)c1 |r| Show InChI InChI=1S/C26H31N7O2/c1-27-24-16-28-15-23(30-24)19-13-22(26(35)29-14-19)31-25(34)18-6-8-20(9-7-18)33-12-4-5-21(33)17-32-10-2-3-11-32/h6-9,13-16,21H,2-5,10-12,17H2,1H3,(H,27,30)(H,29,35)(H,31,34)/t21-/m0/s1 | PDB
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| >1.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Vertex Pharmaceuticals (Europe) Ltd.
Curated by ChEMBL
| Assay Description
Inhibition of IR |
J Med Chem 54: 2341-50 (2011)
Article DOI: 10.1021/jm101499u
BindingDB Entry DOI: 10.7270/Q2KH0NPW |
More data for this
Ligand-Target Pair | |
Insulin receptor
(Homo sapiens (Human)) | BDBM50463483
(CHEMBL4245242)Show SMILES O=C(Cc1cccc(OCCCC2CCNCC2)c1)Nc1nc(cs1)-c1c[nH]c2ncccc12 Show InChI InChI=1S/C26H29N5O2S/c32-24(31-26-30-23(17-34-26)22-16-29-25-21(22)7-2-10-28-25)15-19-4-1-6-20(14-19)33-13-3-5-18-8-11-27-12-9-18/h1-2,4,6-7,10,14,16-18,27H,3,5,8-9,11-13,15H2,(H,28,29)(H,30,31,32) | PDB
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| Article
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| >2.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Vertex Pharmaceuticals Inc
Curated by ChEMBL
| Assay Description
Inhibition of INSR (unknown origin) |
Bioorg Med Chem Lett 28: 2622-2626 (2018)
Article DOI: 10.1016/j.bmcl.2018.06.040
BindingDB Entry DOI: 10.7270/Q2ZC85HX |
More data for this
Ligand-Target Pair | |
Insulin receptor
(Homo sapiens (Human)) | BDBM50463479
(CHEMBL4249925)Show SMILES CS(=O)(=O)Nc1cccc(CC(=O)Nc2nc(cs2)-c2c[nH]c3ncccc23)c1 Show InChI InChI=1S/C19H17N5O3S2/c1-29(26,27)24-13-5-2-4-12(8-13)9-17(25)23-19-22-16(11-28-19)15-10-21-18-14(15)6-3-7-20-18/h2-8,10-11,24H,9H2,1H3,(H,20,21)(H,22,23,25) | PDB
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| >2.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Vertex Pharmaceuticals Inc
Curated by ChEMBL
| Assay Description
Inhibition of INSR (unknown origin) |
Bioorg Med Chem Lett 28: 2622-2626 (2018)
Article DOI: 10.1016/j.bmcl.2018.06.040
BindingDB Entry DOI: 10.7270/Q2ZC85HX |
More data for this
Ligand-Target Pair | |
Insulin receptor
(Homo sapiens (Human)) | BDBM15236
(3,5,7-trihydroxy-2-(3,4,5-trihydroxyphenyl)-4H-chr...)Show SMILES Oc1cc(O)c2c(c1)oc(-c1cc(O)c(O)c(O)c1)c(O)c2=O Show InChI InChI=1S/C15H10O8/c16-6-3-7(17)11-10(4-6)23-15(14(22)13(11)21)5-1-8(18)12(20)9(19)2-5/h1-4,16-20,22H | PDB
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| 2.60E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description
Inhibition of insulin receptor |
J Nat Prod 55: 1529-1560 (1992)
Article DOI: 10.1021/np50089a001
BindingDB Entry DOI: 10.7270/Q2J966CC |
More data for this
Ligand-Target Pair | |
Insulin receptor
(Homo sapiens (Human)) | BDBM50237710
(4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifl...)Show SMILES Cc1cn(cn1)-c1cc(NC(=O)c2ccc(C)c(Nc3nccc(n3)-c3cccnc3)c2)cc(c1)C(F)(F)F Show InChI InChI=1S/C28H22F3N7O/c1-17-5-6-19(10-25(17)37-27-33-9-7-24(36-27)20-4-3-8-32-14-20)26(39)35-22-11-21(28(29,30)31)12-23(13-22)38-15-18(2)34-16-38/h3-16H,1-2H3,(H,35,39)(H,33,36,37) | PDB
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| 4.10E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Genomics Institute of the Novartis Research Foundation
Curated by PDSP Ki Database
| |
Proc Natl Acad Sci U S A 103: 3153-8 (2006)
Article DOI: 10.1073/pnas.0511292103
BindingDB Entry DOI: 10.7270/Q21Z430B |
More data for this
Ligand-Target Pair | |
Insulin receptor
(Homo sapiens (Human)) | BDBM50224883
(7-chloro-3-oxo-8-[(thiazol-5-ylmethyl)-amino]-11,1...)Show SMILES Clc1cc2NC(=O)Nc3cnc(C#N)c(OCCCCOc2cc1NCc1cncs1)n3 Show InChI InChI=1S/C20H18ClN7O3S/c21-13-5-15-17(6-14(13)24-9-12-8-23-11-32-12)30-3-1-2-4-31-19-16(7-22)25-10-18(27-19)28-20(29)26-15/h5-6,8,10-11,24H,1-4,9H2,(H2,26,27,28,29) | PDB
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| >5.24E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Abbott Laboratories
Curated by ChEMBL
| Assay Description
Inhibition of INSR |
Bioorg Med Chem Lett 17: 6593-601 (2007)
Article DOI: 10.1016/j.bmcl.2007.09.063
BindingDB Entry DOI: 10.7270/Q2X067WT |
More data for this
Ligand-Target Pair | |
Insulin receptor
(Homo sapiens (Human)) | BDBM50181669
(5-benzo[1,3]dioxol-5-yl-2-oxo-1,2-dihydro-pyridine...)Show SMILES CN1CCN(Cc2ccc(NC(=O)c3cc(c[nH]c3=O)-c3ccc4OCOc4c3)cc2)CC1 Show InChI InChI=1S/C25H26N4O4/c1-28-8-10-29(11-9-28)15-17-2-5-20(6-3-17)27-25(31)21-12-19(14-26-24(21)30)18-4-7-22-23(13-18)33-16-32-22/h2-7,12-14H,8-11,15-16H2,1H3,(H,26,30)(H,27,31) | PDB
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| 5.30E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
ChemBridge Research Laboratories and ChemBridge Corporation
Curated by ChEMBL
| Assay Description
Inhibitory activity against IRK |
J Med Chem 49: 1006-15 (2006)
Article DOI: 10.1021/jm050824x
BindingDB Entry DOI: 10.7270/Q2H994T6 |
More data for this
Ligand-Target Pair | |
Insulin receptor
(Homo sapiens (Human)) | BDBM50181670
(5-benzo[1,3]dioxol-5-yl-2-oxo-1,2-dihydro-pyridine...)Show SMILES CN1CCN(CC1)c1ccc(NC(=O)c2cc(c[nH]c2=O)-c2ccc3OCOc3c2)cc1 Show InChI InChI=1S/C24H24N4O4/c1-27-8-10-28(11-9-27)19-5-3-18(4-6-19)26-24(30)20-12-17(14-25-23(20)29)16-2-7-21-22(13-16)32-15-31-21/h2-7,12-14H,8-11,15H2,1H3,(H,25,29)(H,26,30) | PDB
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| 8.80E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
ChemBridge Research Laboratories and ChemBridge Corporation
Curated by ChEMBL
| Assay Description
Inhibitory activity against IRK |
J Med Chem 49: 1006-15 (2006)
Article DOI: 10.1021/jm050824x
BindingDB Entry DOI: 10.7270/Q2H994T6 |
More data for this
Ligand-Target Pair | |
Insulin receptor
(Homo sapiens (Human)) | BDBM50181675
(5-benzo[1,3]dioxol-5-yl-2-oxo-1,2-dihydro-pyridine...)Show SMILES CN1CCN(CCCc2ccc(NC(=O)c3cc(c[nH]c3=O)-c3ccc4OCOc4c3)cc2)CC1 Show InChI InChI=1S/C27H30N4O4/c1-30-11-13-31(14-12-30)10-2-3-19-4-7-22(8-5-19)29-27(33)23-15-21(17-28-26(23)32)20-6-9-24-25(16-20)35-18-34-24/h4-9,15-17H,2-3,10-14,18H2,1H3,(H,28,32)(H,29,33) | PDB
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| 9.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
ChemBridge Research Laboratories and ChemBridge Corporation
Curated by ChEMBL
| Assay Description
Inhibitory activity against IRK |
J Med Chem 49: 1006-15 (2006)
Article DOI: 10.1021/jm050824x
BindingDB Entry DOI: 10.7270/Q2H994T6 |
More data for this
Ligand-Target Pair | |
Insulin receptor
(Homo sapiens (Human)) | BDBM13530
(4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[...)Show SMILES CN1CCN(Cc2ccc(cc2)C(=O)Nc2ccc(C)c(Nc3nccc(n3)-c3cccnc3)c2)CC1 Show InChI InChI=1S/C29H31N7O/c1-21-5-10-25(18-27(21)34-29-31-13-11-26(33-29)24-4-3-12-30-19-24)32-28(37)23-8-6-22(7-9-23)20-36-16-14-35(2)15-17-36/h3-13,18-19H,14-17,20H2,1-2H3,(H,32,37)(H,31,33,34) | PDB
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| >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Genomics Institute of the Novartis Research Foundation
Curated by PDSP Ki Database
| |
Proc Natl Acad Sci U S A 103: 3153-8 (2006)
Article DOI: 10.1073/pnas.0511292103
BindingDB Entry DOI: 10.7270/Q21Z430B |
More data for this
Ligand-Target Pair | |
Insulin receptor
(Homo sapiens (Human)) | BDBM50011995
((Hydroxy-naphthalen-2-yl-methyl)-phosphonic acid |...)Show InChI InChI=1S/C11H11O4P/c12-11(16(13,14)15)10-6-5-8-3-1-2-4-9(8)7-10/h1-7,13-16H | PDB
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| 9.50E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Athenex Inc.
Curated by ChEMBL
| Assay Description
Non-competitive inhibition of human placental insulin receptor expressed in CHO cell membrane assessed as decrease in insulin-stimulated A2 phosphory... |
J Med Chem 61: 4704-4719 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00164
BindingDB Entry DOI: 10.7270/Q2Z89GT1 |
More data for this
Ligand-Target Pair | |
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