Found 23 hits Enz. Inhib. hit(s) with Target = 'Receptor-type tyrosine-protein kinase FLT3 [R834Q]' 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 |
|---|
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM247371
(US9447092, 1)Show SMILES Cc1nn(C)cc1-c1nc2c(N3CCN(Cc4ccc(Cl)cc4)CC3)c(Cl)cnc2[nH]1 Show InChI InChI=1S/C22H23Cl2N7/c1-14-17(13-29(2)28-14)21-26-19-20(18(24)11-25-22(19)27-21)31-9-7-30(8-10-31)12-15-3-5-16(23)6-4-15/h3-6,11,13H,7-10,12H2,1-2H3,(H,25,26,27) | PDB
UniProtKB/SwissProt
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UniChem
| US Patent
| n/a | n/a | n/a | 110 | n/a | n/a | n/a | n/a | n/a |
CANCER RESEARCH TECHNOLOGY LIMITED
US Patent
| Assay Description
The kinase selectivity was assessed by profiling Example 1 in a 442-kinase panel (386 non-mutant kinases) at a concentration of 1 μM using the K... |
US Patent US9447092 (2016)
BindingDB Entry DOI: 10.7270/Q2PV6J9C |
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Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621165
(Exemplary Synthetic Procedure #38 | US20230303563...)Show SMILES F[C@H]1CNC[C@@H]1Nc1cccc(n1)-c1cnc2cc(ccn12)C1CC1 |r| | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 0.390 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM538658
(NCGC 00249373 | US11254667, Compound I-17 | US1154...) | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | n/a | 3.40 | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Table 7 For most assays, kinase-tagged T7 phage strains were prepared in an E. coli host derived from the BL21 strain. E. coli were grown to log-phas... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2154MW8 |
More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM185149
(1-[2-[5-[(3-methyloxetan-3-yl)methoxy]benzimidazol...)Show SMILES CC1(COc2ccc3n(cnc3c2)-c2ccc3cccc(N4CCC(N)CC4)c3n2)COC1 Show InChI InChI=1S/C26H29N5O2/c1-26(14-32-15-26)16-33-20-6-7-22-21(13-20)28-17-31(22)24-8-5-18-3-2-4-23(25(18)29-24)30-11-9-19(27)10-12-30/h2-8,13,17,19H,9-12,14-16,27H2,1H3 | PDB
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PC cid
PC sid
PDB
UniChem
| US Patent
| n/a | n/a | n/a | 1.30 | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Table 7 For most assays, kinase-tagged T7 phage strains were prepared in an E. coli host derived from the BL21 strain. E. coli were grown to log-phas... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2154MW8 |
More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM538619
(NCGC 00371479 | US11254667, Compound I-22 | US1154...)Show SMILES COc1cc2ncc(-c3cccc(NC4CCNC4)n3)n2cc1-c1cccnc1 | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | n/a | 0.420 | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Table 7 For most assays, kinase-tagged T7 phage strains were prepared in an E. coli host derived from the BL21 strain. E. coli were grown to log-phas... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2154MW8 |
More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM538621
(NCGC 00371481 | US11254667, Compound I-24 | US1154...)Show SMILES Cn1cc(cn1)-c1cn2c(cnc2cc1CO)-c1cccc(NC2CCNC2)n1 | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | n/a | 0.300 | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Table 7 For most assays, kinase-tagged T7 phage strains were prepared in an E. coli host derived from the BL21 strain. E. coli were grown to log-phas... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2154MW8 |
More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621080
(N-(6-(6-(1-methyl- cyclopropyl)imidazo- [1,2-a]pyr...)Show SMILES CC1(CC1)c1ccc2ncc(-c3cccc(NC4CCC5(CNC5)C4)n3)n2c1 | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 0.800 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621098
(6-(6-(difluorometh- oxy)imidazo[1,2-a]- pyridin-3-...)Show SMILES FC(F)Oc1ccc2ncc(-c3cccc(N[C@H]4CNC[C@@H]4F)n3)n2c1 |r| | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 0.150 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621166
(N-((3S,4S)-4-fluoro- pyrrolidin-3-yl)-6-(6-(1- met...)Show SMILES Cn1cc(cn1)-c1ccc2ncc(-c3cccc(N[C@H]4CNC[C@@H]4F)n3)n2c1 |r| | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 0.540 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621167
(1-(4-(3-(6-(((3S,4S)-4- fluoropyrrolidin-3-yl)- am...)Show SMILES CC(C)(O)Cn1cc(cn1)-c1ccc2ncc(-c3cccc(N[C@H]4CNC[C@@H]4F)n3)n2c1 |r| | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 0.970 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621168
(6-(6-(1-cyclopropyl-1H- pyrazol-4-yl)imidazo- [1,2...)Show SMILES F[C@H]1CNC[C@@H]1Nc1cccc(n1)-c1cnc2ccc(cn12)-c1cnn(c1)C1CC1 |r| | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 1.30 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621115
(US20230303563, Compound 117)Show SMILES OCc1cc2ncc(-c3cccc(N[C@H]4CNC[C@@H]4F)n3)n2cc1C1CC1 |r| | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 0.0610 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621116
(2-(3-(6-(((3S,4S)-4- fluoropyrrolidin-3- yl)amino)...)Show SMILES CC(C)(O)c1cn2c(cnc2cc1CO)-c1cccc(N[C@H]2CNC[C@@H]2F)n1 |r| | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 0.390 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621117
(2-(3-(6-(((3S,4S)-4- fluoropiperidin-3- yl)amino)p...)Show SMILES CC(C)(O)c1cn2c(cnc2cc1CO)-c1cccc(N[C@H]2CNCC[C@@H]2F)n1 |r| | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 0.330 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621123
(US20230303563, Compound 165)Show SMILES FC(F)c1ccc2ncc(-c3cccc(N[C@H]4CNC[C@@H]4F)n3)n2c1 |r| | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 0.890 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621125
((R)-N-(6-(6- (difluoromethyl)imidazo[1,2- a]pyridi...)Show SMILES FC(F)c1ccc2ncc(-c3cccc(N[C@H]4CNCC44CC4)n3)n2c1 |r| | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 0.900 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621126
(6-(6- (difluoromethyl)imidazo[1,2- a]pyridin-3-yl)...)Show SMILES FC(F)c1ccc2ncc(-c3cccc(N[C@H]4CNC[C@@H]4C(F)(F)F)n3)n2c1 |r| | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 0.0360 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621169
(6-(6- (difluoromethyl)imidazo[1,2- a]pyridin-3-yl)...)Show SMILES CC1(C)NCCC1Nc1cccc(n1)-c1cnc2ccc(cn12)C(F)F | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 0.200 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621130
(N-(6-(6- (difluoromethyl)imidazo[1,2- a]pyridin-3-...)Show SMILES FC(F)c1ccc2ncc(-c3cccc(NC4CCC5(CNC5)C4)n3)n2c1 | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 0.340 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621136
(3,5-difluoro-N-((3S,4S)-4- fluoropyrrolidin-3-yl)-...)Show SMILES CC(C)Oc1ccn2c(cnc2c1)-c1nc(N[C@H]2CNC[C@@H]2F)c(F)cc1F |r| | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 8.5 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621137
(3,5-difluoro-N-((3S,4S)-4- fluoropiperidin-3-yl)-6...)Show SMILES CC(C)Oc1ccn2c(cnc2c1)-c1nc(N[C@H]2CNCC[C@@H]2F)c(F)cc1F |r| | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 1.5 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM621161
(N-((3S,4S)-4- fluoropyrrolidin-3-yl)-6-(7- isoprop...)Show SMILES CC(C)Oc1ccn2c(cnc2c1)-c1cccc(N[C@H]2CNC[C@@H]2F)n1 |r| | PDB
UniProtKB/SwissProt
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | n/a | 1.20 | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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Ligand-Target Pair | |
Receptor-type tyrosine-protein kinase FLT3 [R834Q]
(Homo sapiens (Human)) | BDBM50300690
(1-(5-Tert-Butyl-1,2-Oxazol-3-Yl)-3-(4-{7-[2-(Morph...)Show SMILES CC(C)(C)c1cc(NC(=O)Nc2ccc(cc2)-c2cn3c(n2)sc2cc(OCCN4CCOCC4)ccc32)no1 Show InChI InChI=1S/C29H32N6O4S/c1-29(2,3)25-17-26(33-39-25)32-27(36)30-20-6-4-19(5-7-20)22-18-35-23-9-8-21(16-24(23)40-28(35)31-22)38-15-12-34-10-13-37-14-11-34/h4-9,16-18H,10-15H2,1-3H3,(H2,30,32,33,36) | PDB
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US Patent
| n/a | n/a | n/a | 12 | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Table 7 For most assays, kinase-tagged T7 phage strains were prepared in an E. coli host derived from the BL21 strain. E. coli were grown to log-phas... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2154MW8 |
More data for this
Ligand-Target Pair | 
3D Structure (crystal) |
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