Compile Data Set for Download or QSAR
Report error Found 1790 Enz. Inhib. hit(s) with Target = 'Insulin receptor'
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM31095(5-[(Z)-(5-fluoranyl-2-oxidanylidene-1H-indol-3-yli...)
Affinity DataKd:  1.20E+3nMAssay Description:Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2011
Entry Details
PCBioAssay
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM31096(CHEMBL290084 | Staurosporine | cid_451705 | US2024...)
Affinity DataKd:  110nMAssay Description:Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2011
Entry Details
PCBioAssay
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM4814(SUNITINIB MALATE | CHEMBL535 | N-[2-(diethylamino)...)
Affinity DataKd:  500nMAssay Description:Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2011
Entry Details
PCBioAssay
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM13534(VX680 | N-[4-[[4-(4-methylpiperazino)-6-[(5-methyl...)
Affinity DataKd:  630nMAssay Description:Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2011
Entry Details
PCBioAssay
TargetInsulin receptor substrate 1 [1-264](Human)
The University of Texas System

US Patent
LigandPNGBDBM223477(US9320734, 316)
Affinity DataKd:  1.99E+3nMAssay Description:KT1 PH domain small molecule inhibitors were identified using the crystal structure of the AKT1 PH domain bound by PtdIns(1,3,4,5)P4 as descried in T...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/1/2017
Entry Details
US Patent

TargetInsulin receptor substrate 1 [1-264](Human)
The University of Texas System

US Patent
LigandPNGBDBM223486(US9320734, 331)
Affinity DataKd:  2.40E+3nMAssay Description:KT1 PH domain small molecule inhibitors were identified using the crystal structure of the AKT1 PH domain bound by PtdIns(1,3,4,5)P4 as descried in T...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/1/2017
Entry Details
US Patent

TargetInsulin receptor substrate 1 [1-264](Human)
The University of Texas System

US Patent
LigandPNGBDBM223488(US9320734, 332)
Affinity DataKd:  1.07E+4nMAssay Description:KT1 PH domain small molecule inhibitors were identified using the crystal structure of the AKT1 PH domain bound by PtdIns(1,3,4,5)P4 as descried in T...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/1/2017
Entry Details
US Patent

TargetInsulin receptor substrate 1 [1-264](Human)
The University of Texas System

US Patent
LigandPNGBDBM223487(US9320734, 333)
Affinity DataKd:  1.80E+3nMAssay Description:KT1 PH domain small molecule inhibitors were identified using the crystal structure of the AKT1 PH domain bound by PtdIns(1,3,4,5)P4 as descried in T...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/1/2017
Entry Details
US Patent

TargetInsulin receptor substrate 1 [1-264](Human)
The University of Texas System

US Patent
LigandPNGBDBM223489(US9320734, 360)
Affinity DataKd:  1.07E+4nMAssay Description:KT1 PH domain small molecule inhibitors were identified using the crystal structure of the AKT1 PH domain bound by PtdIns(1,3,4,5)P4 as descried in T...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/1/2017
Entry Details
US Patent

TargetInsulin receptor substrate 1 [1-264](Human)
The University of Texas System

US Patent
LigandPNGBDBM223490(US9320734, 335)
Affinity DataKd:  520nMAssay Description:KT1 PH domain small molecule inhibitors were identified using the crystal structure of the AKT1 PH domain bound by PtdIns(1,3,4,5)P4 as descried in T...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/1/2017
Entry Details
US Patent

TargetInsulin receptor substrate 1 [1-264](Human)
The University of Texas System

US Patent
LigandPNGBDBM223477(US9320734, 316)
Affinity DataKd:  390nMAssay Description:KT1 PH domain small molecule inhibitors were identified using the crystal structure of the AKT1 PH domain bound by PtdIns(1,3,4,5)P4 as descried in T...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/1/2017
Entry Details
US Patent

TargetInsulin receptor substrate 1 [1-264](Human)
The University of Texas System

US Patent
LigandPNGBDBM223487(US9320734, 333)
Affinity DataKd:  140nMAssay Description:KT1 PH domain small molecule inhibitors were identified using the crystal structure of the AKT1 PH domain bound by PtdIns(1,3,4,5)P4 as descried in T...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/1/2017
Entry Details
US Patent

TargetInsulin receptor substrate 1 [1-264](Human)
The University of Texas System

US Patent
LigandPNGBDBM223489(US9320734, 360)
Affinity DataKd:  1.74E+3nMAssay Description:KT1 PH domain small molecule inhibitors were identified using the crystal structure of the AKT1 PH domain bound by PtdIns(1,3,4,5)P4 as descried in T...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/1/2017
Entry Details
US Patent

TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM313084(US10166216, Compound 63 | 1-(6-fluoroquinazolin-4-...)
Affinity DataEC50:  126nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50269384(CHEMBL4095081)
Affinity DataEC50:  2.75E+3nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM313069(US10166216, Compound 48 | 1-(6-chloroquinazolin-4-...)
Affinity DataEC50:  14nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM313081(US10166216, Compound 60 | 1-(2-chloro-7-methylthie...)
Affinity DataEC50:  582nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50269375(CHEMBL4086420)
Affinity DataEC50:  1.01E+3nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM313027(N-{2-[(4aR,6S,8aR)-2-amino-6-methyl-4,4a,5,6-tetra...)
Affinity DataEC50:  241nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50269393(CHEMBL4078564)
Affinity DataEC50:  300nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM313086(US10166216, Compound 65 | 1-(2-methylquinazolin-4-...)
Affinity DataEC50:  320nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM313080(US10166216, Compound 59 | N3-(3-chloro-4-(2-(pyrro...)
Affinity DataEC50:  4.17E+3nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM313137(US10166216, Compound 168 | 1-(6,7-dimethoxyquinazo...)
Affinity DataEC50:  1.32E+3nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50269389(CHEMBL4069483)
Affinity DataEC50:  4.58E+3nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM313124(US10166216, Compound 153 | 1-(6,7-dimethoxyquinazo...)
Affinity DataEC50:  1.80E+3nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50269390(CHEMBL4080190)
Affinity DataEC50:  5.03E+3nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50269391(CHEMBL4059790)
Affinity DataEC50: >1.00E+4nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM313140(US10166216, Compound 171 | 1-(6,7-dimethoxyquinazo...)
Affinity DataEC50:  4.76E+3nMAssay Description:Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50459972(CHEMBL4226003)
Affinity DataKd:  0.0200nMAssay Description:Displacement of [TyrA14-125I]-human insulin from human insulin receptor isoform A expressed in baby hamster kidney cells after 2 days by gamma counti...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetInsulin receptor(Mouse)
University of Melbourne

Curated by ChEMBL
LigandPNGBDBM50459972(CHEMBL4226003)
Affinity DataEC50:  4nMAssay Description:Agonist activity at B6D2F1 mouse insulin receptor assessed as increase in glucose incorporation into lipid phase after 2 hrs in presence of D-[3-3H]g...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50505541(CHEMBL4465866)
Affinity DataKd:  1.86E+3nMAssay Description:Binding affinity to recombinant full-length N-terminal His-FLAG-GST-tagged INSR (unknown origin) (1005 to 1310 residues) expressed in baculovirus inf...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50505542(CHEMBL4576489)
Affinity DataKd:  1.69E+3nMAssay Description:Binding affinity to recombinant full-length N-terminal His-FLAG-GST-tagged INSR (unknown origin) (1005 to 1310 residues) expressed in baculovirus inf...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50506238(CHEMBL4457859)
Affinity DataEC50:  4nMAssay Description:Agonist activity at human IR-beta signalling expressed in mouse 3T3 cells assessed as AKT phosphorylation at Ser473 residue after 30 mins by HTRF ass...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50526296(CHEMBL4449858)
Affinity DataKd:  190nMAssay Description:Binding affinity to human INSR (997 to 1318 residues) expressed in mammalian expression system by kinome scan-based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50092148(2-Benzo[b]thiophen-3-yl-3,6-dihydroxy-5-phenyl-[1,...)
Affinity DataEC50:  1.00E+3nMAssay Description:Activation of human insulin receptor tyrosine kinase (IRTK)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50092149(2-[2-(1,1-Dimethyl-allyl)-1H-indol-3-yl]-3,6-dihyd...)
Affinity DataEC50:  5.00E+3nMAssay Description:Activation of human insulin receptor tyrosine kinase (IRTK)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50092146(2-Benzofuran-3-yl-3,6-dihydroxy-5-phenyl-[1,4]benz...)
Affinity DataEC50:  1.50E+3nMAssay Description:Activation of human insulin receptor tyrosine kinase (IRTK)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50092147(2,5-Dihydroxy-3-naphthalen-1-yl-6-phenyl-[1,4]benz...)
Affinity DataEC50:  6.00E+3nMAssay Description:Activation of human insulin receptor tyrosine kinase (IRTK)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50092143(2,5-Dihydroxy-3-(1H-indol-3-yl)-6-phenyl-[1,4]benz...)
Affinity DataEC50:  300nMAssay Description:Activation of human insulin receptor tyrosine kinase (IRTK)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50092145(2,5-Dihydroxy-3-naphthalen-2-yl-6-phenyl-[1,4]benz...)
Affinity DataEC50:  3.00E+4nMAssay Description:Activation of human insulin receptor tyrosine kinase (IRTK)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50092144(2,5-Dihydroxy-3-(1H-indol-3-yl)-6-(7-methyl-1H-ind...)
Affinity DataEC50:  7.00E+3nMAssay Description:Activation of human insulin receptor tyrosine kinase (IRTK)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50092150(2,5-Dihydroxy-3-(1-methyl-1H-indol-3-yl)-6-phenyl-...)
Affinity DataEC50:  300nMAssay Description:Activation of human insulin receptor tyrosine kinase (IRTK)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50548047(CHEMBL4753825)
Affinity DataEC50:  12nMAssay Description:Activation of human IR-B expressed in mouse NIH3T3 cells assessed as increase in Akt phosphorylation at Ser473 residue incubated for 30 mins by HTRF ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50548048(CHEMBL4764550)
Affinity DataEC50:  12nMAssay Description:Activation of human IR-B expressed in mouse NIH3T3 cells assessed as increase in Akt phosphorylation at Ser473 residue incubated for 30 mins by HTRF ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50548049(CHEMBL4751178)
Affinity DataEC50:  12nMAssay Description:Activation of human IR-B expressed in mouse NIH3T3 cells assessed as increase in Akt phosphorylation at Ser473 residue incubated for 30 mins by HTRF ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50548050(CHEMBL4762540)
Affinity DataEC50:  12nMAssay Description:Activation of human IR-B expressed in mouse NIH3T3 cells assessed as increase in Akt phosphorylation at Ser473 residue incubated for 30 mins by HTRF ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50548051(CHEMBL4748140)
Affinity DataEC50:  12nMAssay Description:Activation of human IR-B expressed in mouse NIH3T3 cells assessed as increase in Akt phosphorylation at Ser473 residue incubated for 30 mins by HTRF ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM50587680(CHEMBL5182271)
Affinity DataKd:  12nMAssay Description:Binding affinity to human InsR expressed in mouse IGF1R knockout MEF cells assessed as dissociation constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/18/2023
Entry Details
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM4814(SUNITINIB MALATE | CHEMBL535 | N-[2-(diethylamino)...)
Affinity DataKd:  180nMAssay Description:Average Binding Constant for INSR; NA=Not Active at 10 uMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetInsulin receptor(Human)
Ambit Biosciences

Curated by PubChem BioAssay
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataKd:  73nMAssay Description:Average Binding Constant for INSR; NA=Not Active at 10 uMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
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