Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMXJB4N)

Drug Name
BMS-536924 Drug Info
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
135440466
ChEBI ID
CHEBI:91454
CAS Number
CAS 468740-43-4
TTD Drug ID
DMXJB4N

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Albendazole monooxygenase (CYP3A4) TTXV4FI CP3A4_HUMAN Inhibitor [2]
Cyclin-dependent kinase 2 (CDK2) TT7HF4W CDK2_HUMAN Inhibitor [1]
ERBB2 messenger RNA (HER2 mRNA) TTR5TV4 ERBB2_HUMAN Inhibitor [1]
Extracellular signal-regulated kinase 2 (ERK2) TT4TQBX MK01_HUMAN Inhibitor [1]
Focal adhesion kinase 1 (FAK) TTON5IT FAK1_HUMAN Inhibitor [1]
G1/S-specific cyclin-E1 (CCNE1) TTCEJ4F CCNE1_HUMAN Inhibitor [1]
Insulin-like growth factor I receptor (IGF1R) TTHRID2 IGF1R_HUMAN Inhibitor [3]
LCK tyrosine protein kinase (LCK) TT860QF LCK_HUMAN Inhibitor [1]
Platelet-derived growth factor receptor alpha (PDGFRA) TT8FYO9 PGFRA_HUMAN Inhibitor [1]
Platelet-derived growth factor receptor beta (PDGFRB) TTI7421 PGFRB_HUMAN Inhibitor [1]
Proto-oncogene c-Met (MET) TTNDSF4 MET_HUMAN Inhibitor [1]
RAC-alpha serine/threonine-protein kinase (AKT1) TTWTSCV AKT1_HUMAN Inhibitor [1]
Vascular endothelial growth factor receptor 2 (KDR) TTUTJGQ VGFR2_HUMAN Inhibitor [1]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Albendazole monooxygenase (CYP3A4) DTT CYP3A4 11.692 6.58 4.984 9.089
RAC-alpha serine/threonine-protein kinase (AKT1) DTT AKT1 7.399 7.276 7.816 6.959
Proto-oncogene c-Met (MET) DTT MET 6.737 6.293 7.744 6.879
Platelet-derived growth factor receptor beta (PDGFRB) DTT PDGFRB 6.43 6.333 6.671 5.97
Insulin-like growth factor I receptor (IGF1R) DTT IGF1R 4.542 5.508 6.35 5.558
Platelet-derived growth factor receptor alpha (PDGFRA) DTT PDGFRA 6.189 7.636 7.84 7.086
LCK tyrosine protein kinase (LCK) DTT LCK 5.2 4.443 4.53 6.325
Extracellular signal-regulated kinase 2 (ERK2) DTT MAPK1 5.848 6.896 7.236 6.465
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Discovery agent
ICD Disease Classification N.A.
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Vascular endothelial growth factor receptor 2 (KDR) DTT KDR 1.98E-01 0.11 0.2
Proto-oncogene c-Met (MET) DTT MET 1.08E-03 -0.24 -0.4
Platelet-derived growth factor receptor beta (PDGFRB) DTT PDGFRB 5.35E-10 0.36 0.89
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitum... J Med Chem. 2005 Sep 8;48(18):5639-43.
2 Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)py... J Med Chem. 2008 Oct 9;51(19):5897-900.
3 SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1744-8.