General
Preferred name
FALNIDAMOL
Synonyms
BIBX 1382 dihydrochloride ()
Falnidamol dihydrochloride ()
BIBX 1382 ()
BIBX-1382 ()
BIBX1382 ()
Bibx 1382 ()
P&D ID
PD012960
CAS
1216920-18-1
196612-93-8
Tags
available
nuisance
drug candidate
probe
Drug indication
Chronic lymphocytic leukaemia
Drug Status
investigational
Max Phase
Phase 1
Probe info
Probe selectivity
protein-selective
Probe type
calculated probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
105
No orthogonal probes found
Similar probes
6
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Falnidamol is a selective and reversible inhibitor of EGFR and HER2.
(GtoPdb)
DESCRIPTION
Falnidamol, also known as BIBX 1382, is a pyrimido-pyrimidine with antitumor activity. BIBX 1382 inhibits the intracellular tyrosine kinase domain of the Epidermal Growth Factor Receptor (EGFR) thus specifically reversing the aberrant enzymatic activity from overexpressed and constitutively activated EGFR, and subsequently inhibiting cell proliferation and inducing cell differentiation.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Negative control of LY 294002 (Cat. No. 1130)
(Tocris Bioactive Compound Library)
DESCRIPTION
Highly selective EGFR-kinase inhibitor
(Tocriscreen Plus)
DESCRIPTION
Highly selective EGFR-kinase inhibitor
(Tocriscreen Total)
DESCRIPTION
BIBX 1382 dihydrochloride is a potent and selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC50 = 3 nM) with > 1000-fold lower potency than ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM). BIBX 1382 inhibits Lassa, Ebola and Marburg viruses.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
4
Compound Sets
18
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugMAP
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
Nuisance compounds in cellular assays
Probe Miner (suitable probes)
ReFrame library
Selleckchem Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
Tocriscreen Total
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
38
Molecular Weight
387.14
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
3
cLogP
3.46
TPSA
78.86
Fraction CSP3
0.33
Chiral centers
0.0
Largest ring
6.0
QED
0.71
Structural alerts
1
Beta lactamase activation
Nuisance compounds in cellular assays
Related compounds
Custom attributes
(extracted from source data)
Target Type
Enzyme-Linked Receptors
Primary Target
EGFR
MOA
Inhibitor
EGFR inhibitor
Target
EGFR, ERBB2
EGFR,p38 MAPK
Pathway
JAK/STAT Signaling
Protein Tyrosine Kinase/RTK
Source data
