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-UHFFFAOYSA-N

Data  19 IC50  1 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 20 hits for monomerid = 14459   

TargetDimer of Protein farnesyltransferase subunit beta(Human)
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50: 10nMAssay Description:Effect on Ras processing in Cos-1 monkey kidney cells expressing either H-Ras-Val 12-CVLS or H-Ras-Val12.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGTPase KRas(Human)
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50: 40nMAssay Description:Inhibition of K-Ras in human NCI-H460 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2024
Entry Details
PubMed
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of human GGTase1 in human Burkitt lymphoma (Daudi) cell supernatant using [3H]geranylgeranylMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2020
Entry Details Article
PubMed
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
In Depth
Date in BDB:
9/2/2020
Entry Details Article
PubMed
TargetGeranylgeranyl transferase type-1 subunit beta(Rat)
Temple University

Curated by ChEMBL
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of rat brain GGTase1 assessed as decrease in transfer of [3H]H]geranylgeranyl from [3H]geranylgeranyl PPi to H-Ras-CVLL after 30 mins by l...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
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
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50: 7.80nMAssay Description:In vitro inhibitory activity against farnesyltransferase (FTase)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetATP-dependent translocase ABCB1(Human)
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50: 2.70E+3nMAssay Description:TP_TRANSPORTER: inhibition of DNR efflux (DNR: uM) in MDR1-expressing NIH3T3 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details
PubMed
TargetDimer of Protein farnesyltransferase subunit beta(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:Inhibitory concentration against farnesyltransferase was determinedMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed
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
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetATP-dependent RNA helicase RhlE(Vibrio fischeri (strain ATCC 700601 / ES114))
University of Washington At Seattle

LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50: 250nMAssay Description:Assays for PFT activity were performed with a PFT-specific scintillation assay (SPA) kit (Amersham Biosciences, Piscataway, NJ). IC50 values were cal...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/23/2007
Entry Details Article
PubMed
TargetDimer of Protein farnesyltransferase subunit beta(Human)
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50: 2nMAssay Description:Inhibition of [3H]FPP incorporation into H-ras CVLS by FarnesyltransferaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetDimer of Protein farnesyltransferase subunit beta(Human)
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50: 5.00E+5nMAssay Description:Inhibition of K-Ras transformed NIH3T3 cell proliferationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM14459((+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of Bovine geranylgeranyltransferase (GGT)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
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
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetDimer of Protein farnesyltransferase subunit beta(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 Protein farnesyltransferase in Cos-1 monkey kidney cells expressing H-Ras-valMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
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
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetDimer of Protein farnesyltransferase subunit beta(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 Farnesyl protein transferaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetDimer of Protein farnesyltransferase subunit beta(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:Inhibitory activity against Hras Farnesyltransferase (FPT).More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
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
In Depth
Date in BDB:
3/26/2007
Entry Details Article
PubMed