BDBM14459 (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(R)-yl)-1-piperidin-yl]-2-oxo-ethyl]-1-piperidinecarboxamide::4-(2-{4-[(2R)-6,15-dibromo-13-chloro-4-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,12,14-hexaen-2-yl]piperidin-1-yl}-2-oxoethyl)piperidine-1-carboxamide::CHEMBL298734::Lonafarnib::SCH 66336::Sarasar

SMILES NC(=O)N1CCC(CC(=O)N2CCC(CC2)[C@H]2c3ncc(Br)cc3CCc3cc(Cl)cc(Br)c23)CC1

InChI Key InChIKey=DHMTURDWPRKSOA-RUZDIDTESA-N

Data  18 IC50  1 EC50

PDB links: 2 PDB IDs match this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 7 hits for monomerid = 14459   

TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50:  1.90E+3nMAssay Description:In vitro inhibition of human FarnesyltransferaseMore data for this Ligand-Target Pair
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50:  8.30nMAssay Description:Inhibition of Bovine farnesyltransferase (FTase)More data for this Ligand-Target Pair
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataEC50:  100nMAssay Description:Inhibition of Ras farnesylation in H-Ras transformed NIH3T3 cellsMore data for this Ligand-Target Pair
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50:  7.80nMAssay Description:In vitro inhibitory activity of the compound against farnesyltransferase (FTase)More data for this Ligand-Target Pair
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of rat brain FTase assessed as decrease in transfer of [3H]farnesyl from [3H]farnesyl PPi to H-Ras-CVLS after 30 mins by liquid scintillat...More data for this Ligand-Target Pair
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of human recombinant FTase using [3H]farnesyldiphosphateMore data for this Ligand-Target Pair
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50:  1.90nMpH: 7.5 T: 2°CAssay Description:FPT activity was determined by measuring transfer of [3H] farnesyl from [3H]farnesyl pyrophosphate to the substrate His6-Ha-Ras-CVLS. The incorporate...More data for this Ligand-Target Pair