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PubMed code 9822558

Compile data set for download or QSAR
Found 25 hits of Enzyme Inhibition Constant Data   
Target/Host
(Institution)
LigandTarget/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
pHTemp
°C
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14457
PNG
((+)-4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo...)
Show SMILES [O-][n+]1ccc(CC(=O)N2CCC(CC2)[C@H]2c3ncc(Br)cc3CCc3cc(Cl)cc(Br)c23)cc1 |r|
Show InChI InChI=1S/C26H24Br2ClN3O2/c27-20-12-19-2-1-18-13-21(29)14-22(28)24(18)25(26(19)30-15-20)17-5-7-31(8-6-17)23(33)11-16-3-9-32(34)10-4-16/h3-4,9-10,12-15,17,25H,1-2,5-8,11H2/t25-/m1/s1
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n/an/a 1.30n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14461
PNG
((+)-4-(3,10-Dibromo-8-chloro-6,11-dihydro-5H-benzo...)
Show SMILES [O-][n+]1ccc(CC(=O)N2CCN(CC2)[C@H]2c3ncc(Br)cc3CCc3cc(Cl)cc(Br)c23)cc1 |r|
Show InChI InChI=1S/C25H23Br2ClN4O2/c26-19-12-18-2-1-17-13-20(28)14-21(27)23(17)25(24(18)29-15-19)31-9-7-30(8-10-31)22(33)11-16-3-5-32(34)6-4-16/h3-6,12-15,25H,1-2,7-11H2/t25-/m1/s1
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n/an/a 1.80n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14459
PNG
((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Show SMILES NC(=O)N1CCC(CC(=O)N2CCC(CC2)[C@H]2c3ncc(Br)cc3CCc3cc(Cl)cc(Br)c23)CC1 |r|
Show InChI InChI=1S/C27H31Br2ClN4O2/c28-20-12-19-2-1-18-13-21(30)14-22(29)24(18)25(26(19)32-15-20)17-5-9-33(10-6-17)23(35)11-16-3-7-34(8-4-16)27(31)36/h12-17,25H,1-11H2,(H2,31,36)/t25-/m1/s1
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n/an/a 1.90n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14473
PNG
((-)-1-(8-Chloro-3,7-dibromo-6,11-dihydro-5H-benzo-...)
Show SMILES [O-][n+]1ccc(CC(=O)N2CCN(CC2)[C@H]2c3ccc(Cl)c(Br)c3CCc3cc(Br)cnc23)cc1 |r|
Show InChI InChI=1S/C25H23Br2ClN4O2/c26-18-14-17-1-2-19-20(3-4-21(28)23(19)27)25(24(17)29-15-18)31-11-9-30(10-12-31)22(33)13-16-5-7-32(34)8-6-16/h3-8,14-15,25H,1-2,9-13H2/t25-/m0/s1
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n/an/a 2.30n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14467
PNG
((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Show SMILES NC(=O)N1CCC(CC(=O)N2CCN(CC2)[C@H]2c3ncc(Br)cc3CCc3cc(Cl)cc(Br)c23)CC1 |r|
Show InChI InChI=1S/C26H30Br2ClN5O2/c27-19-12-18-2-1-17-13-20(29)14-21(28)23(17)25(24(18)31-15-19)33-9-7-32(8-10-33)22(35)11-16-3-5-34(6-4-16)26(30)36/h12-16,25H,1-11H2,(H2,30,36)/t25-/m1/s1
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n/an/a 2.5n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14469
PNG
((-)-4-(8-Chloro-3,7-dibromo-6,11-dihydro-5H-benzo-...)
Show SMILES [O-][n+]1ccc(CC(=O)N2CCC(CC2)[C@H]2c3ccc(Cl)c(Br)c3CCc3cc(Br)cnc23)cc1 |r|
Show InChI InChI=1S/C26H24Br2ClN3O2/c27-19-14-18-1-2-21-20(3-4-22(29)25(21)28)24(26(18)30-15-19)17-7-9-31(10-8-17)23(33)13-16-5-11-32(34)12-6-16/h3-6,11-12,14-15,17,24H,1-2,7-10,13H2/t24-/m0/s1
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n/an/a 2.60n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14477
PNG
((-)-4-[2-[4-(3,7-Dibromo-8-chloro-6,11-dihydro-5Hb...)
Show SMILES NC(=O)N1CCC(CC(=O)N2CCN(CC2)[C@H]2c3ccc(Cl)c(Br)c3CCc3cc(Br)cnc23)CC1 |r|
Show InChI InChI=1S/C26H30Br2ClN5O2/c27-18-14-17-1-2-19-20(3-4-21(29)23(19)28)25(24(17)31-15-18)33-11-9-32(10-12-33)22(35)13-16-5-7-34(8-6-16)26(30)36/h3-4,14-16,25H,1-2,5-13H2,(H2,30,36)/t25-/m0/s1
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n/an/a 3.10n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14463
PNG
((+)-4-(3-Bromo-8,10-dichloro-6,11-dihydro-5H-benzo...)
Show SMILES [O-][n+]1ccc(CC(=O)N2CCN(CC2)[C@H]2c3ncc(Br)cc3CCc3cc(Cl)cc(Cl)c23)cc1 |r|
Show InChI InChI=1S/C25H23BrCl2N4O2/c26-19-12-18-2-1-17-13-20(27)14-21(28)23(17)25(24(18)29-15-19)31-9-7-30(8-10-31)22(33)11-16-3-5-32(34)6-4-16/h3-6,12-15,25H,1-2,7-11H2/t25-/m1/s1
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n/an/a<3.80n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14471
PNG
((-)-4-[2-[4-(3,7-Dibromo-8-chloro-6,11-dihydro-5H-...)
Show SMILES NC(=O)N1CCC(CC(=O)N2CCC(CC2)[C@H]2c3ccc(Cl)c(Br)c3CCc3cc(Br)cnc23)CC1 |r|
Show InChI InChI=1S/C27H31Br2ClN4O2/c28-19-14-18-1-2-21-20(3-4-22(30)25(21)29)24(26(18)32-15-19)17-7-11-33(12-8-17)23(35)13-16-5-9-34(10-6-16)27(31)36/h3-4,14-17,24H,1-2,5-13H2,(H2,31,36)/t24-/m0/s1
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n/an/a 5n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14475
PNG
((-)-1-(3-Bromo-7,8-dichloro-6,11-dihydro-5H-benzo-...)
Show SMILES [O-][n+]1ccc(CC(=O)N2CCN(CC2)[C@H]2c3ccc(Cl)c(Cl)c3CCc3cc(Br)cnc23)cc1 |r|
Show InChI InChI=1S/C25H23BrCl2N4O2/c26-18-14-17-1-2-19-20(3-4-21(27)23(19)28)25(24(17)29-15-18)31-11-9-30(10-12-31)22(33)13-16-5-7-32(34)8-6-16/h3-8,14-15,25H,1-2,9-13H2/t25-/m0/s1
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n/an/a 6n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14465
PNG
((+)-4-(3-Bromo-8-chloro-10-fluoro-6,11-dihydro-5H-...)
Show SMILES [O-][n+]1ccc(CC(=O)N2CCN(CC2)[C@H]2c3ncc(Br)cc3CCc3cc(Cl)cc(F)c23)cc1 |r|
Show InChI InChI=1S/C25H23BrClFN4O2/c26-19-12-18-2-1-17-13-20(27)14-21(28)23(17)25(24(18)29-15-19)31-9-7-30(8-10-31)22(33)11-16-3-5-32(34)6-4-16/h3-6,12-15,25H,1-2,7-11H2/t25-/m1/s1
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n/an/a 16.7n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14466
PNG
((-)-4-(3-Bromo-8-chloro-10-fluoro-6,11-dihydro-5H-...)
Show SMILES [O-][n+]1ccc(CC(=O)N2CCN(CC2)[C@@H]2c3ncc(Br)cc3CCc3cc(Cl)cc(F)c23)cc1 |r|
Show InChI InChI=1S/C25H23BrClFN4O2/c26-19-12-18-2-1-17-13-20(27)14-21(28)23(17)25(24(18)29-15-19)31-9-7-30(8-10-31)22(33)11-16-3-5-32(34)6-4-16/h3-6,12-15,25H,1-2,7-11H2/t25-/m0/s1
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n/an/a 33.1n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14456
PNG
(4-N-carboxamidopiperidinylacetyl 2 | 4-[2-(4-{6-br...)
Show SMILES NC(=O)N1CCC(CC(=O)N2CCN(CC2)C2c3ccc(Cl)cc3CCc3cc(Br)cnc23)CC1
Show InChI InChI=1S/C26H31BrClN5O2/c27-20-14-19-2-1-18-15-21(28)3-4-22(18)25(24(19)30-16-20)32-11-9-31(10-12-32)23(34)13-17-5-7-33(8-6-17)26(29)35/h3-4,14-17,25H,1-2,5-13H2,(H2,29,35)
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n/an/a 49n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14470
PNG
((+)-4-(8-Chloro-3,7-dibromo-6,11-dihydro-5H-benzo-...)
Show SMILES [O-][n+]1ccc(CC(=O)N2CCC(CC2)[C@@H]2c3ccc(Cl)c(Br)c3CCc3cc(Br)cnc23)cc1 |r|
Show InChI InChI=1S/C26H24Br2ClN3O2/c27-19-14-18-1-2-21-20(3-4-22(29)25(21)28)24(26(18)30-15-19)17-7-9-31(10-8-17)23(33)13-16-5-11-32(34)12-6-16/h3-6,11-12,14-15,17,24H,1-2,7-10,13H2/t24-/m1/s1
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n/an/a 62n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14472
PNG
((+)-4-[2-[4-(3,7-Dibromo-8-chloro-6,11-dihydro-5H-...)
Show SMILES NC(=O)N1CCC(CC(=O)N2CCC(CC2)[C@@H]2c3ccc(Cl)c(Br)c3CCc3cc(Br)cnc23)CC1 |r|
Show InChI InChI=1S/C27H31Br2ClN4O2/c28-19-14-18-1-2-21-20(3-4-22(30)25(21)29)24(26(18)32-15-19)17-7-11-33(12-8-17)23(35)13-16-5-9-34(10-6-16)27(31)36/h3-4,14-17,24H,1-2,5-13H2,(H2,31,36)/t24-/m1/s1
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n/an/a 78n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14476
PNG
(3-bromo-8-chloro-7-fluoro-11-{4-[(1-oxidopyridin-4...)
Show SMILES [O-][n+]1ccc(CC(=O)N2CCN(CC2)C2c3ccc(Cl)c(F)c3CCc3cc(Br)cnc23)cc1
Show InChI InChI=1S/C25H23BrClFN4O2/c26-18-14-17-1-2-19-20(3-4-21(27)23(19)28)25(24(17)29-15-18)31-11-9-30(10-12-31)22(33)13-16-5-7-32(34)8-6-16/h3-8,14-15,25H,1-2,9-13H2
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n/an/a 86n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14458
PNG
((-)-4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo...)
Show SMILES [O-][n+]1ccc(CC(=O)N2CCC(CC2)[C@@H]2c3ncc(Br)cc3CCc3cc(Cl)cc(Br)c23)cc1 |r|
Show InChI InChI=1S/C26H24Br2ClN3O2/c27-20-12-19-2-1-18-13-21(29)14-22(28)24(18)25(26(19)30-15-20)17-5-7-31(8-6-17)23(33)11-16-3-9-32(34)10-4-16/h3-4,9-10,12-15,17,25H,1-2,5-8,11H2/t25-/m0/s1
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n/an/a>88n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14455
PNG
(3-bromo-4-pyridylacetyl N-oxide 1 | 4-[2-(4-{6-bro...)
Show SMILES [#8-]-[n+]1ccc(-[#6]-[#6](=O)-[#7]-2-[#6]-[#6]\[#6](-[#6]-[#6]-2)=[#6]-2/c3ccc(Cl)cc3-[#6]-[#6]-c3cc(Br)cnc-23)cc1
Show InChI InChI=1S/C26H23BrClN3O2/c27-21-14-20-2-1-19-15-22(28)3-4-23(19)25(26(20)29-16-21)18-7-9-30(10-8-18)24(32)13-17-5-11-31(33)12-6-17/h3-6,11-12,14-16H,1-2,7-10,13H2
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n/an/a 90n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14460
PNG
((-)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Show SMILES NC(=O)N1CCC(CC(=O)N2CCC(CC2)[C@@H]2c3ncc(Br)cc3CCc3cc(Cl)cc(Br)c23)CC1 |r|
Show InChI InChI=1S/C27H31Br2ClN4O2/c28-20-12-19-2-1-18-13-21(30)14-22(29)24(18)25(26(19)32-15-20)17-5-9-33(10-6-17)23(35)11-16-3-7-34(8-4-16)27(31)36/h12-17,25H,1-11H2,(H2,31,36)/t25-/m0/s1
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n/an/a>94n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14468
PNG
((-)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Show SMILES NC(=O)N1CCC(CC(=O)N2CCN(CC2)[C@@H]2c3ncc(Br)cc3CCc3cc(Cl)cc(Br)c23)CC1 |r|
Show InChI InChI=1S/C26H30Br2ClN5O2/c27-19-12-18-2-1-17-13-20(29)14-21(28)23(17)25(24(18)31-15-19)33-9-7-32(8-10-33)22(35)11-16-3-5-34(6-4-16)26(30)36/h12-16,25H,1-11H2,(H2,30,36)/t25-/m0/s1
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n/an/a>94n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14462
PNG
((-)-4-(3,10-Dibromo-8-chloro-6,11-dihydro-5H-benzo...)
Show SMILES [O-][n+]1ccc(CC(=O)N2CCN(CC2)[C@@H]2c3ncc(Br)cc3CCc3cc(Cl)cc(Br)c23)cc1 |r|
Show InChI InChI=1S/C25H23Br2ClN4O2/c26-19-12-18-2-1-17-13-20(28)14-21(27)23(17)25(24(18)29-15-19)31-9-7-30(8-10-31)22(33)11-16-3-5-32(34)6-4-16/h3-6,12-15,25H,1-2,7-11H2/t25-/m0/s1
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n/an/a>95n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14474
PNG
((+)-1-(8-Chloro-3,7-dibromo-6,11-dihydro-5H-benzo-...)
Show SMILES [O-][n+]1ccc(CC(=O)N2CCN(CC2)[C@@H]2c3ccc(Cl)c(Br)c3CCc3cc(Br)cnc23)cc1 |r|
Show InChI InChI=1S/C25H23Br2ClN4O2/c26-18-14-17-1-2-19-20(3-4-21(28)23(19)27)25(24(17)29-15-18)31-11-9-30(10-12-31)22(33)13-16-5-7-32(34)8-6-16/h3-8,14-15,25H,1-2,9-13H2/t25-/m1/s1
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n/an/a>99n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14464
PNG
((-)-4-(3-Bromo-8,10-dichloro-6,11-dihydro-5H-benzo...)
Show SMILES [O-][n+]1ccc(CC(=O)N2CCN(CC2)[C@@H]2c3ncc(Br)cc3CCc3cc(Cl)cc(Cl)c23)cc1 |r|
Show InChI InChI=1S/C25H23BrCl2N4O2/c26-19-12-18-2-1-17-13-20(27)14-21(28)23(17)25(24(18)29-15-19)31-9-7-30(8-10-31)22(33)11-16-3-5-32(34)6-4-16/h3-6,12-15,25H,1-2,7-11H2/t25-/m0/s1
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n/an/a>110n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14454
PNG
(1-(4-pyridylacetyl)-4-(8-chloro-5,6-dihydro-11H-be...)
Show SMILES Clc1ccc2c(-[#6]-[#6]-c3cccnc3\[#6]-2=[#6]-2\[#6]-[#6]-[#7](-[#6]-[#6]-2)-[#6](=O)-[#6]-c2ccncc2)c1
Show InChI InChI=1S/C26H24ClN3O/c27-22-5-6-23-21(17-22)4-3-20-2-1-11-29-26(20)25(23)19-9-14-30(15-10-19)24(31)16-18-7-12-28-13-8-18/h1-2,5-8,11-13,17H,3-4,9-10,14-16H2
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n/an/a 250n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha


(Homo sapiens (Human))
BDBM14478
PNG
((+)-4-[2-[4-(3,7-Dibromo-8-chloro-6,11-dihydro-5Hb...)
Show SMILES NC(=O)N1CCC(CC(=O)N2CCN(CC2)[C@@H]2c3ccc(Cl)c(Br)c3CCc3cc(Br)cnc23)CC1 |r|
Show InChI InChI=1S/C26H30Br2ClN5O2/c27-18-14-17-1-2-19-20(3-4-21(29)23(19)28)25(24(17)31-15-18)33-11-9-32(10-12-33)22(35)13-16-5-7-34(8-6-16)26(30)36/h3-4,14-16,25H,1-2,5-13H2,(H2,30,36)/t25-/m1/s1
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n/an/a>280n/an/an/an/a7.522



Schering-Plough Research Institute



Assay Description
FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...


J Med Chem 41: 4890-902 (1998)


Article DOI: 10.1021/jm980462b
BindingDB Entry DOI: 10.7270/Q2ZS2TRS
More data for this
Ligand-Target Pair
* indicates data uncertainty>20%