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Compile Data Set for Download or QSAR

Found 1315 hits Enz. Inhib. hit(s) with Target = 'VEGFR-1 (Flt-1)' AND taxid = 9606   
Target
(Institution)
LigandTarget
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
pHTemp
°C
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM4814
PNG
(CHEMBL535 | N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fl...)
Show SMILES CCN(CC)CCNC(=O)c1c(C)[nH]c(\C=C2/C(=O)Nc3ccc(F)cc23)c1C
Show InChI InChI=1S/C22H27FN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-
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PubMed
2n/an/an/an/an/an/an/an/a



Qilu Pharmaceutical Co, Ltd

Curated by ChEMBL


Assay Description
Binding affinity to VEGFR1 (unknown origin)


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50402020
PNG
(CHEMBL2205426)
Show SMILES CC(C)(C)Nc1c(Nc2ccnc(Nc3ccc(cc3)-c3ccncc3)n2)c(=O)c1=O
Show InChI InChI=1S/C23H22N6O2/c1-23(2,3)29-19-18(20(30)21(19)31)27-17-10-13-25-22(28-17)26-16-6-4-14(5-7-16)15-8-11-24-12-9-15/h4-13,29H,1-3H3,(H2,25,26,27,28)
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14n/an/an/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibition of recombinant FLT1 after 1 hr by scintillation counter analysis in presence of gamma-[33P]ATP


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50184807
PNG
((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-me...)
Show SMILES C[C@@H](O)COc1cn2ncnc(Oc3ccc4[nH]c(C)cc4c3F)c2c1C
Show InChI InChI=1S/C19H19FN4O3/c1-10-6-13-14(23-10)4-5-15(17(13)20)27-19-18-12(3)16(26-8-11(2)25)7-24(18)22-9-21-19/h4-7,9,11,23,25H,8H2,1-3H3/t11-/m1/s1
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60n/an/an/an/an/an/an/an/a



Pharmaceutical Research Institute

Curated by ChEMBL


Assay Description
Inhibitory activity against VEGFR1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221531
PNG
(6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)-4-...)
Show SMILES COc1cc2c(N[C@@H]3C[C@H]3c3ccccc3)c(cnc2cc1OCCCN1CCN(C)CC1)C#N
Show InChI InChI=1S/C28H33N5O2/c1-32-10-12-33(13-11-32)9-6-14-35-27-17-24-23(16-26(27)34-2)28(21(18-29)19-30-24)31-25-15-22(25)20-7-4-3-5-8-20/h3-5,7-8,16-17,19,22,25H,6,9-15H2,1-2H3,(H,30,31)/t22-,25+/m0/s1
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110n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221516
PNG
(6-methoxy-7-(3-morpholinopropoxy)-4-((1R,2S)-2-phe...)
Show SMILES COc1cc2c(N[C@@H]3C[C@H]3c3ccccc3)c(cnc2cc1OCCCN1CCOCC1)C#N
Show InChI InChI=1S/C27H30N4O3/c1-32-25-15-22-23(16-26(25)34-11-5-8-31-9-12-33-13-10-31)29-18-20(17-28)27(22)30-24-14-21(24)19-6-3-2-4-7-19/h2-4,6-7,15-16,18,21,24H,5,8-14H2,1H3,(H,29,30)/t21-,24+/m0/s1
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350n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50224883
PNG
(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)
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>440n/an/an/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibition of FLT1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221527
PNG
(7-methoxy-6-(3-morpholinopropoxy)-4-((1R,2S)-2-phe...)
Show SMILES COc1cc2ncc(C#N)c(N[C@@H]3C[C@H]3c3ccccc3)c2cc1OCCCN1CCOCC1
Show InChI InChI=1S/C27H30N4O3/c1-32-25-16-23-22(15-26(25)34-11-5-8-31-9-12-33-13-10-31)27(20(17-28)18-29-23)30-24-14-21(24)19-6-3-2-4-7-19/h2-4,6-7,15-16,18,21,24H,5,8-14H2,1H3,(H,29,30)/t21-,24+/m0/s1
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910n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221529
PNG
(7-(4-(morpholinomethyl)phenyl)-4-((1R,2S)-2-phenyl...)
Show SMILES N#Cc1cnc2cc(ccc2c1N[C@@H]1C[C@H]1c1ccccc1)-c1ccc(CN2CCOCC2)cc1
Show InChI InChI=1S/C30H28N4O/c31-18-25-19-32-28-16-24(22-8-6-21(7-9-22)20-34-12-14-35-15-13-34)10-11-26(28)30(25)33-29-17-27(29)23-4-2-1-3-5-23/h1-11,16,19,27,29H,12-15,17,20H2,(H,32,33)/t27-,29+/m0/s1
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920n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50020310
PNG
(CHEMBL3288854)
Show SMILES CN1CCN(CCC(=O)Nc2c(C)[nH]c(\C=C3/C(=O)Nc4ccc(F)cc34)c2C)CC1
Show InChI InChI=1S/C23H28FN5O2/c1-14-20(13-18-17-12-16(24)4-5-19(17)26-23(18)31)25-15(2)22(14)27-21(30)6-7-29-10-8-28(3)9-11-29/h4-5,12-13,25H,6-11H2,1-3H3,(H,26,31)(H,27,30)/b18-13-
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1.10E+3n/an/an/an/an/an/an/an/a



Qilu Pharmaceutical Co, Ltd

Curated by ChEMBL


Assay Description
Binding affinity to VEGFR1 (unknown origin)


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221522
PNG
(6-(4-(aminomethyl)phenyl)-4-((1R,2S)-2-phenylcyclo...)
Show SMILES NCc1ccc(cc1)-c1ccc2ncc(C#N)c(N[C@@H]3C[C@H]3c3ccccc3)c2c1
Show InChI InChI=1S/C26H22N4/c27-14-17-6-8-18(9-7-17)20-10-11-24-23(12-20)26(21(15-28)16-29-24)30-25-13-22(25)19-4-2-1-3-5-19/h1-12,16,22,25H,13-14,27H2,(H,29,30)/t22-,25+/m0/s1
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1.40E+3n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221519
PNG
(6-methoxy-7-(1-methylpiperidin-4-yloxy)-4-((1R,2S)...)
Show SMILES COc1cc2c(N[C@@H]3C[C@H]3c3ccccc3)c(cnc2cc1OC1CCN(C)CC1)C#N
Show InChI InChI=1S/C26H28N4O2/c1-30-10-8-19(9-11-30)32-25-14-22-21(13-24(25)31-2)26(18(15-27)16-28-22)29-23-12-20(23)17-6-4-3-5-7-17/h3-7,13-14,16,19-20,23H,8-12H2,1-2H3,(H,28,29)/t20-,23+/m0/s1
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1.50E+3n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221518
PNG
(6,7-dimethoxy-4-((1R,2S)-2-phenylcyclopropylamino)...)
Show SMILES COc1cc2ncc(C#N)c(N[C@@H]3C[C@H]3c3ccccc3)c2cc1OC
Show InChI InChI=1S/C21H19N3O2/c1-25-19-9-16-17(10-20(19)26-2)23-12-14(11-22)21(16)24-18-8-15(18)13-6-4-3-5-7-13/h3-7,9-10,12,15,18H,8H2,1-2H3,(H,23,24)/t15-,18+/m0/s1
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1.60E+3n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221528
PNG
(7-methoxy-4-((1R,2S)-2-phenylcyclopropylamino)-6-(...)
Show SMILES COc1cc2ncc(C#N)c(N[C@@H]3C[C@H]3c3ccccc3)c2cc1OCCCc1cccnc1
Show InChI InChI=1S/C28H26N4O2/c1-33-26-15-24-23(14-27(26)34-12-6-8-19-7-5-11-30-17-19)28(21(16-29)18-31-24)32-25-13-22(25)20-9-3-2-4-10-20/h2-5,7,9-11,14-15,17-18,22,25H,6,8,12-13H2,1H3,(H,31,32)/t22-,25+/m0/s1
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1.71E+3n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221524
PNG
(6-methoxy-4-((1R,2S)-2-phenylcyclopropylamino)-7-(...)
Show SMILES COc1cc2c(N[C@@H]3C[C@H]3c3ccccc3)c(cnc2cc1OCCCc1cccnc1)C#N
Show InChI InChI=1S/C28H26N4O2/c1-33-26-14-23-24(15-27(26)34-12-6-8-19-7-5-11-30-17-19)31-18-21(16-29)28(23)32-25-13-22(25)20-9-3-2-4-10-20/h2-5,7,9-11,14-15,17-18,22,25H,6,8,12-13H2,1H3,(H,31,32)/t22-,25+/m0/s1
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1.90E+3n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221517
PNG
(6-methoxy-7-(2-methoxyethoxy)-4-((1R,2S)-2-phenylc...)
Show SMILES COCCOc1cc2ncc(C#N)c(N[C@@H]3C[C@H]3c3ccccc3)c2cc1OC
Show InChI InChI=1S/C23H23N3O3/c1-27-8-9-29-22-12-19-18(11-21(22)28-2)23(16(13-24)14-25-19)26-20-10-17(20)15-6-4-3-5-7-15/h3-7,11-12,14,17,20H,8-10H2,1-2H3,(H,25,26)/t17-,20+/m0/s1
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2.90E+3n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221521
PNG
(7-methoxy-6-(2-morpholinoethoxy)-4-((1R,2S)-2-phen...)
Show SMILES COc1cc2ncc(C#N)c(N[C@@H]3C[C@H]3c3ccccc3)c2cc1OCCN1CCOCC1
Show InChI InChI=1S/C26H28N4O3/c1-31-24-15-22-21(14-25(24)33-12-9-30-7-10-32-11-8-30)26(19(16-27)17-28-22)29-23-13-20(23)18-5-3-2-4-6-18/h2-6,14-15,17,20,23H,7-13H2,1H3,(H,28,29)/t20-,23+/m0/s1
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>1.00E+4n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221526
PNG
(6-methoxy-4-((1R,2S)-2-phenylcyclopropylamino)quin...)
Show SMILES COc1ccc2ncc(C#N)c(N[C@@H]3C[C@H]3c3ccccc3)c2c1
Show InChI InChI=1S/C20H17N3O/c1-24-15-7-8-18-17(9-15)20(14(11-21)12-22-18)23-19-10-16(19)13-5-3-2-4-6-13/h2-9,12,16,19H,10H2,1H3,(H,22,23)/t16-,19+/m0/s1
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>1.00E+4n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221515
PNG
(6-(benzyloxy)-7-methoxy-4-((1R,2S)-2-phenylcyclopr...)
Show SMILES COc1cc2ncc(C#N)c(N[C@@H]3C[C@H]3c3ccccc3)c2cc1OCc1ccccc1
Show InChI InChI=1S/C27H23N3O2/c1-31-25-14-23-22(13-26(25)32-17-18-8-4-2-5-9-18)27(20(15-28)16-29-23)30-24-12-21(24)19-10-6-3-7-11-19/h2-11,13-14,16,21,24H,12,17H2,1H3,(H,29,30)/t21-,24+/m0/s1
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>1.00E+4n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221520
PNG
(6-(3-(morpholinomethyl)phenyl)-4-((1R,2S)-2-phenyl...)
Show SMILES N#Cc1cnc2ccc(cc2c1N[C@@H]1C[C@H]1c1ccccc1)-c1cccc(CN2CCOCC2)c1
Show InChI InChI=1S/C30H28N4O/c31-18-25-19-32-28-10-9-24(23-8-4-5-21(15-23)20-34-11-13-35-14-12-34)16-27(28)30(25)33-29-17-26(29)22-6-2-1-3-7-22/h1-10,15-16,19,26,29H,11-14,17,20H2,(H,32,33)/t26-,29+/m0/s1
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>1.00E+4n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221523
PNG
(7-methoxy-4-((1R,2S)-2-phenylcyclopropylamino)quin...)
Show SMILES COc1ccc2c(N[C@@H]3C[C@H]3c3ccccc3)c(cnc2c1)C#N
Show InChI InChI=1S/C20H17N3O/c1-24-15-7-8-16-18(9-15)22-12-14(11-21)20(16)23-19-10-17(19)13-5-3-2-4-6-13/h2-9,12,17,19H,10H2,1H3,(H,22,23)/t17-,19+/m0/s1
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>1.00E+4n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50221525
PNG
(6-(4-(morpholinomethyl)phenyl)-4-((1R,2S)-2-phenyl...)
Show SMILES N#Cc1cnc2ccc(cc2c1N[C@@H]1C[C@H]1c1ccccc1)-c1ccc(CN2CCOCC2)cc1
Show InChI InChI=1S/C30H28N4O/c31-18-25-19-32-28-11-10-24(22-8-6-21(7-9-22)20-34-12-14-35-15-13-34)16-27(28)30(25)33-29-17-26(29)23-4-2-1-3-5-23/h1-11,16,19,26,29H,12-15,17,20H2,(H,32,33)/t26-,29+/m0/s1
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>1.00E+4n/an/an/an/an/an/an/an/a



Tanabe Research Laboratories USA, Inc.

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50331095
PNG
(CHEMBL1289494 | Tivozanib)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)Nc4cc(C)on4)c(Cl)c3)c2cc1OC
Show InChI InChI=1S/C22H19ClN4O5/c1-12-8-21(27-32-12)26-22(28)25-16-5-4-13(9-15(16)23)31-18-6-7-24-17-11-20(30-3)19(29-2)10-14(17)18/h4-11H,1-3H3,(H2,25,26,27,28)
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n/an/a 0.210n/an/an/an/an/an/a



University of Genoa

Curated by ChEMBL


Assay Description
Inhibition of VEGFR1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50236362
PNG
(CHEMBL429743 | N-(4-chlorophenyl)-6-(6,7-dimethoxy...)
Show SMILES COc1cc2nccc(Oc3ccc4c(cccc4c3)C(=O)Nc3ccc(Cl)cc3)c2cc1OC
Show InChI InChI=1S/C28H21ClN2O4/c1-33-26-15-23-24(16-27(26)34-2)30-13-12-25(23)35-20-10-11-21-17(14-20)4-3-5-22(21)28(32)31-19-8-6-18(29)7-9-19/h3-16H,1-2H3,(H,31,32)
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n/an/a 0.5n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of VEGFR1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50399540
PNG
(FORETINIB)
Show SMILES COc1cc2c(Oc3ccc(NC(=O)C4(CC4)C(=O)Nc4ccc(F)cc4)cc3F)ccnc2cc1OCCCN1CCOCC1
Show InChI InChI=1S/C34H34F2N4O6/c1-43-30-20-25-27(21-31(30)45-16-2-13-40-14-17-44-18-15-40)37-12-9-28(25)46-29-8-7-24(19-26(29)36)39-33(42)34(10-11-34)32(41)38-23-5-3-22(35)4-6-23/h3-9,12,19-21H,2,10-11,13-18H2,1H3,(H,38,41)(H,39,42)
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n/an/a 0.800n/an/an/an/an/an/a



University of Genoa

Curated by ChEMBL


Assay Description
Inhibition of VEGFR1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50375642
PNG
(CHEMBL406381 | KRN-633)
Show SMILES CCCNC(=O)Nc1ccc(Oc2ncnc3cc(OC)c(OC)cc23)cc1Cl
Show InChI InChI=1S/C20H21ClN4O4/c1-4-7-22-20(26)25-15-6-5-12(8-14(15)21)29-19-13-9-17(27-2)18(28-3)10-16(13)23-11-24-19/h5-6,8-11H,4,7H2,1-3H3,(H2,22,25,26)
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n/an/a 1n/an/an/an/an/an/a



University of Oxford

Curated by ChEMBL


Assay Description
Inhibition of human VEGFR1 in HUVEC cells


Citation and Details
Checked by Author
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50185178
PNG
(1-tert-butyl-3-(3-(5-(4-(piperidin-1-yl)piperidin-...)
Show SMILES CC(C)(C)NC(=O)Nc1ccc2[nH]nc(-c3nc4ccc(cc4[nH]3)N3CCC(CC3)N3CCCCC3)c2c1
Show InChI InChI=1S/C29H38N8O/c1-29(2,3)33-28(38)30-19-7-9-23-22(17-19)26(35-34-23)27-31-24-10-8-21(18-25(24)32-27)37-15-11-20(12-16-37)36-13-5-4-6-14-36/h7-10,17-18,20H,4-6,11-16H2,1-3H3,(H,31,32)(H,34,35)(H2,30,33,38)
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n/an/a 1n/an/an/an/an/an/a



Chiron Corporation

Curated by ChEMBL


Assay Description
Inhibition of VEGFR1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM4814
PNG
(CHEMBL535 | N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fl...)
Show SMILES CCN(CC)CCNC(=O)c1c(C)[nH]c(\C=C2/C(=O)Nc3ccc(F)cc23)c1C
Show InChI InChI=1S/C22H27FN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-
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n/an/a 1n/an/an/an/an/an/a



Exelixis

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST-tagged Flt1 using poly(Glu,Tyr) as substrate after 60 mins by alphascreen assay


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50381716
PNG
(ABT-348 | ILORASERTIB | US8722890, 1 | US8722890, ...)
Show SMILES Nc1ncc(-c2cnn(CCO)c2)c2scc(-c3ccc(NC(=O)Nc4cccc(F)c4)cc3)c12
Show InChI InChI=1S/C25H21FN6O2S/c26-17-2-1-3-19(10-17)31-25(34)30-18-6-4-15(5-7-18)21-14-35-23-20(12-28-24(27)22(21)23)16-11-29-32(13-16)8-9-33/h1-7,10-14,33H,8-9H2,(H2,27,28)(H2,30,31,34)
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n/an/a 1.25n/an/an/an/an/an/a



AbbVie Inc.

US Patent


Assay Description
To determine the activity of the various kinases, a homogenous time-resolved fluorescence (HTRF) in vitro kinase assay was used. (Mathis, G., HTRF(R)...


US Patent US8722890 (2014)

More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM121390
PNG
(US8722890, 5)
Show SMILES COc1ccc(NC(=O)Nc2ccc(cc2)-c2csc3c(cnc(N)c23)-c2cnn(C[C@H](O)CO)c2)cc1
Show InChI InChI=1S/C27H26N6O4S/c1-37-21-8-6-19(7-9-21)32-27(36)31-18-4-2-16(3-5-18)23-15-38-25-22(11-29-26(28)24(23)25)17-10-30-33(12-17)13-20(35)14-34/h2-12,15,20,34-35H,13-14H2,1H3,(H2,28,29)(H2,31,32,36)/t20-/m0/s1
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n/an/a 1.45n/an/an/an/an/an/a



AbbVie Inc.

US Patent


Assay Description
To determine the activity of the various kinases, a homogenous time-resolved fluorescence (HTRF) in vitro kinase assay was used. (Mathis, G., HTRF(R)...


US Patent US8722890 (2014)

More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50381698
PNG
(CHEMBL1969102 | US8722890, 6)
Show SMILES Cc1cccc(NC(=O)Nc2ccc(cc2)-c2csc3c(cnc(N)c23)-c2cn[nH]c2)c1
Show InChI InChI=1S/C24H20N6OS/c1-14-3-2-4-18(9-14)30-24(31)29-17-7-5-15(6-8-17)20-13-32-22-19(16-10-27-28-11-16)12-26-23(25)21(20)22/h2-13H,1H3,(H2,25,26)(H,27,28)(H2,29,30,31)
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n/an/a 1.90n/an/an/an/an/an/a



AbbVie Inc.

US Patent


Assay Description
To determine the activity of the various kinases, a homogenous time-resolved fluorescence (HTRF) in vitro kinase assay was used. (Mathis, G., HTRF(R)...


US Patent US8722890 (2014)

More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM24773
PNG
(AMG 706 | AMG-706 | Motesanib | N-(3,3-dimethyl-1,...)
Show SMILES CC1(C)CNc2cc(NC(=O)c3cccnc3NCc3ccncc3)ccc12
Show InChI InChI=1S/C22H23N5O/c1-22(2)14-26-19-12-16(5-6-18(19)22)27-21(28)17-4-3-9-24-20(17)25-13-15-7-10-23-11-8-15/h3-12,26H,13-14H2,1-2H3,(H,24,25)(H,27,28)
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n/an/a 2n/an/an/an/a7.522



Amgen



Assay Description
In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50137208
PNG
(1-{4-[4-(1H-Indol-5-ylamino)-thieno[3,2-d]pyrimidi...)
Show SMILES NC(=O)C1CCN(Cc2ccc(cc2)-c2cc3ncnc(Nc4ccc5[nH]ccc5c4)c3s2)CC1
Show InChI InChI=1S/C27H26N6OS/c28-26(34)19-8-11-33(12-9-19)15-17-1-3-18(4-2-17)24-14-23-25(35-24)27(31-16-30-23)32-21-5-6-22-20(13-21)7-10-29-22/h1-7,10,13-14,16,19,29H,8-9,11-12,15H2,(H2,28,34)(H,30,31,32)
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n/an/a 2n/an/an/an/an/an/a



Pfizer Global Research and Development

Curated by ChEMBL


Assay Description
Inhibitory activity against Vascular endothelial growth factor receptor


Bioorg Med Chem Lett 14: 21-4 (2003)

More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM4630
PNG
(2-chloro-4-fluoro-5-{[6-methoxy-7-(2-methoxyethoxy...)
Show SMILES COCCOc1cc2ncnc(Nc3cc(O)c(Cl)cc3F)c2cc1OC
Show InChI InChI=1S/C18H17ClFN3O4/c1-25-3-4-27-17-8-13-10(5-16(17)26-2)18(22-9-21-13)23-14-7-15(24)11(19)6-12(14)20/h5-9,24H,3-4H2,1-2H3,(H,21,22,23)
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n/an/a<2n/an/an/an/a7.422



AstraZeneca



Assay Description
An ELISA assay was used to determine the ability of inhibitor to inhibit VEGF-R RTK activity. The compounds were incubated with enzyme 20 min at room...


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50329885
PNG
(4-(6-(4-(2-morpholinoethoxy)phenyl)pyrazolo[1,5-a]...)
Show SMILES Oc1ccc(cc1O)-c1cnn2cc(cnc12)-c1ccc(OCCN2CCOCC2)cc1
Show InChI InChI=1S/C24H24N4O4/c29-22-6-3-18(13-23(22)30)21-15-26-28-16-19(14-25-24(21)28)17-1-4-20(5-2-17)32-12-9-27-7-10-31-11-8-27/h1-6,13-16,29-30H,7-12H2
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n/an/a 2n/an/an/an/an/an/a



Ansaris

Curated by ChEMBL


Assay Description
Inhibition of FLT1 by Hot Spot filtration binding assay


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50210272
PNG
(6-((4-methylpiperazin-1-yl)methyl)-3-(5-(3-phenoxy...)
Show SMILES CN1CCN(Cc2ccc-3c(Cc4c-3n[nH]c4-c3csc(c3)C#CCOc3ccccc3)c2)CC1
Show InChI InChI=1S/C29H28N4OS/c1-32-11-13-33(14-12-32)19-21-9-10-26-22(16-21)18-27-28(30-31-29(26)27)23-17-25(35-20-23)8-5-15-34-24-6-3-2-4-7-24/h2-4,6-7,9-10,16-17,20H,11-15,18-19H2,1H3,(H,30,31)
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n/an/a 2n/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibition of Flt1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM8826
PNG
(3-(4-{4-aminothieno[2,3-d]pyrimidin-5-yl}phenyl)-1...)
Show SMILES Cc1cccc(NC(=O)Nc2ccc(cc2)-c2csc3ncnc(N)c23)c1
Show InChI InChI=1S/C20H17N5OS/c1-12-3-2-4-15(9-12)25-20(26)24-14-7-5-13(6-8-14)16-10-27-19-17(16)18(21)22-11-23-19/h2-11H,1H3,(H2,21,22,23)(H2,24,25,26)
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n/an/a 2n/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibition of FLT1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM24773
PNG
(AMG 706 | AMG-706 | Motesanib | N-(3,3-dimethyl-1,...)
Show SMILES CC1(C)CNc2cc(NC(=O)c3cccnc3NCc3ccncc3)ccc12
Show InChI InChI=1S/C22H23N5O/c1-22(2)14-26-19-12-16(5-6-18(19)22)27-21(28)17-4-3-9-24-20(17)25-13-15-7-10-23-11-8-15/h3-12,26H,13-14H2,1-2H3,(H,24,25)(H,27,28)
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n/an/a 2n/an/an/an/an/an/a



University of Genoa

Curated by ChEMBL


Assay Description
Inhibition of VEGFR1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50185181
PNG
(5-(4-(piperidin-1-yl)piperidin-1-yl)-2-(6-(trifluo...)
Show SMILES FC(F)(F)c1ccc2c(n[nH]c2c1)-c1nc2ccc(cc2[nH]1)N1CCC(CC1)N1CCCCC1
Show InChI InChI=1S/C25H27F3N6/c26-25(27,28)16-4-6-19-21(14-16)31-32-23(19)24-29-20-7-5-18(15-22(20)30-24)34-12-8-17(9-13-34)33-10-2-1-3-11-33/h4-7,14-15,17H,1-3,8-13H2,(H,29,30)(H,31,32)
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Chiron Corporation

Curated by ChEMBL


Assay Description
Inhibition of VEGFR1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM110647
PNG
(US8614234, 115)
Show SMILES Cc1cccc(NC(=O)Nc2ccc(Oc3ccnc(c3)-c3cc(c[nH]3)C(O)=O)cc2)c1
Show InChI InChI=1S/C24H20N4O4/c1-15-3-2-4-18(11-15)28-24(31)27-17-5-7-19(8-6-17)32-20-9-10-25-22(13-20)21-12-16(14-26-21)23(29)30/h2-14,26H,1H3,(H,29,30)(H2,27,28,31)
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n/an/a 2n/an/an/an/an/an/a



Allergan, Inc.

US Patent


Assay Description
Kinase assays were performed in 96 well microtiter plates that were coated overnight with 30.mu.g of poly-Glu-Tyr (4:1) in 10 mM Phosphate Buffered S...


US Patent US8614234 (2013)

More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM121388
PNG
(US8722890, 3)
Show SMILES C[C@H](O)Cn1cc(cn1)-c1cnc(N)c2c(csc12)-c1ccc(NC(=O)Nc2cccc(C)c2)cc1
Show InChI InChI=1S/C27H26N6O2S/c1-16-4-3-5-21(10-16)32-27(35)31-20-8-6-18(7-9-20)23-15-36-25-22(12-29-26(28)24(23)25)19-11-30-33(14-19)13-17(2)34/h3-12,14-15,17,34H,13H2,1-2H3,(H2,28,29)(H2,31,32,35)/t17-/m0/s1
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n/an/a 2.04n/an/an/an/an/an/a



AbbVie Inc.

US Patent


Assay Description
To determine the activity of the various kinases, a homogenous time-resolved fluorescence (HTRF) in vitro kinase assay was used. (Mathis, G., HTRF(R)...


US Patent US8722890 (2014)

More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50381716
PNG
(ABT-348 | ILORASERTIB | US8722890, 1 | US8722890, ...)
Show SMILES Nc1ncc(-c2cnn(CCO)c2)c2scc(-c3ccc(NC(=O)Nc4cccc(F)c4)cc3)c12
Show InChI InChI=1S/C25H21FN6O2S/c26-17-2-1-3-19(10-17)31-25(34)30-18-6-4-15(5-7-18)21-14-35-23-20(12-28-24(27)22(21)23)16-11-29-32(13-16)8-9-33/h1-7,10-14,33H,8-9H2,(H2,27,28)(H2,30,31,34)
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n/an/a 2.10n/an/an/an/an/an/a



AbbVie Inc.

US Patent


Assay Description
To determine the activity of the various kinases, a homogenous time-resolved fluorescence (HTRF) in vitro kinase assay was used. (Mathis, G., HTRF(R)...


US Patent US8722890 (2014)

More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM21079
PNG
(1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-...)
Show SMILES Cc1ccc(F)c(NC(=O)Nc2ccc(cc2)-c2cccc3[nH]nc(N)c23)c1
Show InChI InChI=1S/C21H18FN5O/c1-12-5-10-16(22)18(11-12)25-21(28)24-14-8-6-13(7-9-14)15-3-2-4-17-19(15)20(23)27-26-17/h2-11H,1H3,(H3,23,26,27)(H2,24,25,28)
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n/an/a 3n/an/an/an/a7.522



Abbott Laboratories



Assay Description
The assay uses purified enzyme interacting with biotinylated peptide substrate. HTRF is based on the proximity of europium cryptate (donor fluorophor...


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM228532
PNG
(US9340555, 15)
Show SMILES Cc1ccc(F)c(NC(=O)Nc2ccc(Oc3ccnc4cc(sc34)C(=O)NCCCN3CCCC(CO)C3)cc2)c1
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n/an/a 3n/an/an/an/an/an/a



Allergan, Inc.

US Patent


Assay Description
Kinase assays were performed in 96 well microtiter plates that were coated overnight with 30 μg of poly-Glu-Tyr (4:1) in 10 mM Phosphate Buffered ...


US Patent US9340555 (2016)

More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50137202
PNG
(2-(Methyl-{4-[7-(2-methyl-1H-indol-5-ylamino)-thie...)
Show SMILES CN(CCO)Cc1ccc(cc1)-c1cc2nccc(Nc3ccc4[nH]c(C)cc4c3)c2s1
Show InChI InChI=1S/C26H26N4OS/c1-17-13-20-14-21(7-8-22(20)28-17)29-23-9-10-27-24-15-25(32-26(23)24)19-5-3-18(4-6-19)16-30(2)11-12-31/h3-10,13-15,28,31H,11-12,16H2,1-2H3,(H,27,29)
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n/an/a 3n/an/an/an/an/an/a



Pfizer Global Research and Development

Curated by ChEMBL


Assay Description
Inhibitory activity against Vascular endothelial growth factor receptor


Bioorg Med Chem Lett 14: 21-4 (2003)

More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50137206
PNG
((2-Methyl-1H-indol-5-yl)-(2-{4-[(2-pyridin-1-yl-et...)
Show SMILES Cc1cc2cc(Nc3ccnc4cc(sc34)-c3ccc(CNCCN4CCNCC4)cc3)ccc2[nH]1
Show InChI InChI=1S/C29H32N6S/c1-20-16-23-17-24(6-7-25(23)33-20)34-26-8-9-32-27-18-28(36-29(26)27)22-4-2-21(3-5-22)19-31-12-15-35-13-10-30-11-14-35/h2-9,16-18,30-31,33H,10-15,19H2,1H3,(H,32,34)
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n/an/a 3n/an/an/an/an/an/a



Pfizer Global Research and Development

Curated by ChEMBL


Assay Description
Inhibitory activity against Vascular endothelial growth factor receptor


Bioorg Med Chem Lett 14: 21-4 (2003)

More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM4633
PNG
(2-chloro-4-fluoro-5-{[6-methoxy-7-(2-methoxyethoxy...)
Show SMILES COCCOc1cc2nccc(Nc3cc(O)c(Cl)cc3F)c2cc1OC
Show InChI InChI=1S/C19H18ClFN2O4/c1-25-5-6-27-19-10-15-11(7-18(19)26-2)14(3-4-22-15)23-16-9-17(24)12(20)8-13(16)21/h3-4,7-10,24H,5-6H2,1-2H3,(H,22,23)
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n/an/a 3n/an/an/an/a7.422



AstraZeneca



Assay Description
An ELISA assay was used to determine the ability of inhibitor to inhibit VEGF-R RTK activity. The compounds were incubated with enzyme 20 min at room...


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM25118
PNG
((3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,...)
Show SMILES CN1CCN(CC1)c1ccc2nc([nH]c2c1)-c1c(N)c2c(F)cccc2[nH]c1=O
Show InChI InChI=1S/C21H21FN6O/c1-27-7-9-28(10-8-27)12-5-6-14-16(11-12)25-20(24-14)18-19(23)17-13(22)3-2-4-15(17)26-21(18)29/h2-6,11H,7-10H2,1H3,(H,24,25)(H3,23,26,29)
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n/an/a 3n/an/an/an/an/an/a



Novartis Institutes for Biomedical Research

Curated by ChEMBL


Assay Description
Inhibition of VEGFR1


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50243417
PNG
(1-{4-[7-Amino-3-(1-methyl-1H-pyrazol-4-yl)pyrazolo...)
Show SMILES Cc1cccc(NC(=O)Nc2ccc(cc2)-c2cnc3c(ccn3c2N)-c2cnn(C)c2)c1
Show InChI InChI=1S/C25H23N7O/c1-16-4-3-5-20(12-16)30-25(33)29-19-8-6-17(7-9-19)22-14-27-24-21(10-11-32(24)23(22)26)18-13-28-31(2)15-18/h3-15H,26H2,1-2H3,(H2,29,30,33)
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n/an/a 3n/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibition of Flt1 (unknown origin) by HTRF assay


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM21079
PNG
(1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-...)
Show SMILES Cc1ccc(F)c(NC(=O)Nc2ccc(cc2)-c2cccc3[nH]nc(N)c23)c1
Show InChI InChI=1S/C21H18FN5O/c1-12-5-10-16(22)18(11-12)25-21(28)24-14-8-6-13(7-9-14)15-3-2-4-17-19(15)20(23)27-26-17/h2-11H,1H3,(H3,23,26,27)(H2,24,25,28)
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n/an/a 3n/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibition of FLT1 by HTRF assay


Citation and Details
More data for this
Ligand-Target Pair
VEGFR-1 (Flt-1)


(Homo sapiens (human))
BDBM50185182
PNG
(2-(5-(benzyloxy)-1H-indazol-3-yl)-5-(4-(piperidin-...)
Show SMILES C(Oc1ccc2[nH]nc(-c3nc4ccc(cc4[nH]3)N3CCC(CC3)N3CCCCC3)c2c1)c1ccccc1
Show InChI InChI=1S/C31H34N6O/c1-3-7-22(8-4-1)21-38-25-10-12-27-26(20-25)30(35-34-27)31-32-28-11-9-24(19-29(28)33-31)37-17-13-23(14-18-37)36-15-5-2-6-16-36/h1,3-4,7-12,19-20,23H,2,5-6,13-18,21H2,(H,32,33)(H,34,35)
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n/an/a 3n/an/an/an/an/an/a



Chiron Corporation

Curated by ChEMBL


Assay Description
Inhibition of VEGFR1


Citation and Details
More data for this
Ligand-Target Pair
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