Found 7 hits Enz. Inhib. hit(s) with Target = 'Dimer of Protein farnesyltransferase subunit beta' and Ligand = 'BDBM14459' 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 |
Dimer of Protein farnesyltransferase subunit beta
(Homo sapiens (Human)) | BDBM14459
((+)-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 | PDB
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UniProtKB/SwissProt
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CHEMBL MCE MMDB PC cid PC sid PDB UniChem
Patents
Similars
| PDB Article PubMed
| n/a | n/a | 1.90 | n/a | n/a | n/a | n/a | n/a | n/a |
Schering-Plough Research Institute
Curated by ChEMBL
| Assay Description Inhibitory activity against Hras Farnesyltransferase (FPT). |
J Med Chem 42: 2651-61 (1999)
Article DOI: 10.1021/jm990059k BindingDB Entry DOI: 10.7270/Q2ST7P2V |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Dimer of Protein farnesyltransferase subunit beta
(Homo sapiens (Human)) | BDBM14459
((+)-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 | PDB
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UniProtKB/SwissProt
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CHEMBL MCE MMDB PC cid PC sid PDB UniChem
Patents
Similars
| PDB Article PubMed
| n/a | n/a | 1.90 | n/a | n/a | n/a | n/a | n/a | n/a |
Schering-Plough Research Institute
Curated by ChEMBL
| Assay Description Inhibition of Farnesyl protein transferase |
J Med Chem 42: 2125-35 (1999)
Article DOI: 10.1021/jm990030g BindingDB Entry DOI: 10.7270/Q2ZS2VP9 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Dimer of Protein farnesyltransferase subunit beta
(Homo sapiens (Human)) | BDBM14459
((+)-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 | PDB
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UniProtKB/SwissProt
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CHEMBL MCE MMDB PC cid PC sid PDB UniChem
Patents
Similars
| PDB PubMed
| n/a | n/a | 1.90 | n/a | n/a | n/a | n/a | n/a | n/a |
Schering-Plough Research Institute
Curated by ChEMBL
| Assay Description Inhibition of Protein farnesyltransferase in Cos-1 monkey kidney cells expressing H-Ras-val |
J Med Chem 45: 3854-64 (2002)
BindingDB Entry DOI: 10.7270/Q2TD9WPB |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Dimer of Protein farnesyltransferase subunit beta
(Homo sapiens (Human)) | BDBM14459
((+)-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 | PDB
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CHEMBL MCE MMDB PC cid PC sid PDB UniChem
Patents
Similars
| PDB Article PubMed
| n/a | n/a | 1.90 | n/a | n/a | n/a | n/a | n/a | n/a |
Merck Research Laboratories
Curated by ChEMBL
| Assay Description Inhibitory concentration against farnesyltransferase was determined |
J Med Chem 47: 1869-78 (2004)
Article DOI: 10.1021/jm0305467 BindingDB Entry DOI: 10.7270/Q2RX9CVX |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Dimer of Protein farnesyltransferase subunit beta
(Homo sapiens (Human)) | BDBM14459
((+)-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 | PDB
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CHEMBL MCE MMDB PC cid PC sid PDB UniChem
Patents
Similars
| PDB Article PubMed
| n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
Schering-Plough Research Institute
Curated by ChEMBL
| Assay Description Inhibition of [3H]-FPP incorporation into H-ras CVLS by Farnesyltransferase |
Bioorg Med Chem Lett 14: 5899-902 (2004)
Article DOI: 10.1016/j.bmcl.2004.09.020 BindingDB Entry DOI: 10.7270/Q2PG1R78 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Dimer of Protein farnesyltransferase subunit beta
(Homo sapiens (Human)) | BDBM14459
((+)-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 | PDB
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UniProtKB/SwissProt
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CHEMBL MCE MMDB PC cid PC sid PDB UniChem
Patents
Similars
| PDB Article PubMed
| n/a | n/a | 10 | n/a | n/a | n/a | n/a | n/a | n/a |
Schering-Plough Research Institute
Curated by ChEMBL
| Assay Description Effect on Ras processing in Cos-1 monkey kidney cells expressing either H-Ras-Val 12-CVLS or H-Ras-Val12. |
J Med Chem 42: 2651-61 (1999)
Article DOI: 10.1021/jm990059k BindingDB Entry DOI: 10.7270/Q2ST7P2V |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Dimer of Protein farnesyltransferase subunit beta
(Homo sapiens (Human)) | BDBM14459
((+)-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 | PDB
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UniProtKB/SwissProt
antibodypedia GoogleScholar AffyNet
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CHEMBL MCE MMDB PC cid PC sid PDB UniChem
Patents
Similars
| PDB Article PubMed
| n/a | n/a | 5.00E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
Schering-Plough Research Institute
Curated by ChEMBL
| Assay Description Inhibition of K-Ras transformed NIH3T3 cell proliferation |
Bioorg Med Chem Lett 14: 5899-902 (2004)
Article DOI: 10.1016/j.bmcl.2004.09.020 BindingDB Entry DOI: 10.7270/Q2PG1R78 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |