General
Preferred name
Milciclib Maleate
Synonyms
MILCICLIB ()
PHA-848125 ()
PHA848125, cmpd 28 ()
PHA848125 ()
Milciclib (PHA-848125) ()
PHA 848125 ()
PHA-848125 ()
PHA-848125AC ()
P&D ID
PD010683
CAS
802539-81-7
Tags
available
drug candidate
Drug indication
Hepatocellular carcinoma
Thymic cancer
Neoplasm
Drug Status
investigational
Max Phase
2.0
1.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
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
Milciclib is an orally bioavailable inhibitor of cyclin-dependent kinases (CDKs) and neurotrophic tyrosine kinase, receptor, type 1 (aka TRKA) . It is compound 28 in Brasca et al (2009) .
DESCRIPTION
Milciclib is an orally bioavailable inhibitor of cyclin-dependent kinases (CDKs) and neurotrophic tyrosine kinase, receptor, type 1 (aka TRKA) . It is compound 28 in Brasca et al (2009) . Milciclib exhibits a notable level of promiscuity across the CDKs .
(GtoPdb)
DESCRIPTION
Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
PRICE
174
DESCRIPTION
Milciclib (PHA-848125) (PHA-848125) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. Phase 2.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
5
Organisms
4
Compound Sets
21
Cayman Chemical Bioactives
CDK inhibitor database (CDKiDB)
ChEMBL Drugs
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
The Pathogen Box
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
33
Molecular Weight
460.27
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
2
Rotatable Bonds
4
Ring Count
5
Aromatic Ring Count
3
cLogP
2.57
TPSA
91.21
Fraction CSP3
0.44
Chiral centers
0.0
Largest ring
6.0
QED
0.62
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Disease
KINETOPLASTIDS
Targets
CDK2
Pathway
Autophagy
Cell Cycle/Checkpoint
Tyrosine Kinase/Adaptors
Cell Cycle/DNA Damage
Target
CDK2, CDK4, CDK7, NTRK1
Autophagy,CDK
CDK1
NTRK1
CDK
CDK2/CyclinA
CDK4/CyclinD1
CDK5/p35
CDK7/CyclinH
TrkA
MOA
CDK inhibitor, growth factor receptor inhibitor
Source data
