General
Preferred name
K-252A
Synonyms
SF 2370 ()
K252a ()
SF2370 ()
Antibiotic K 252a ()
Antibiotic SF 2370 ()
P&D ID
PD008176
CAS
97161-97-2
99533-80-9
Tags
available
drug candidate
Drug indication
Solid tumour/cancer
Drug Status
experimental
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION K-252a, a staurosporine analog, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively[1][2]. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene[3].
Compound Sets
7
Cayman Chemical Bioactives
11338
Clinical kinase drugs
CZ-OPENSCREEN Bioactive Library
DrugBank
DB02152
DrugMAP
DMT68RG
MedChem Express Bioactive Compound Library
HY-N6732
Novartis Chemogenetic Library (NIBR MoA Box)
External IDs
30
Properties
(calculated by RDKit )
Molecular Weight
467.15
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
1
Ring Count
8
Aromatic Ring Count
5
cLogP
3.66
TPSA
94.72
Fraction CSP3
0.26
Chiral centers
3.0
Largest ring
7.0
QED
0.37
Structural alerts
1
Nonspecific kinase inhibition
Nuisance compounds
Related compounds
Custom attributes
(extracted from source data)
Targets
PRKCA,PRKCB,PRKCZ,PRKCH,PRKCG,PRKCD,PRKCI,PRKCE
Member status
member
MOA
Leucine-Rich Repeat Kinase 2 (LRRK2
Dardarin) Inhibitors
"Leucine-Rich Repeat Kinase 2 (LRRK2
Dardarin) Inhibitors"
Target
antibiotic
Autophagy
CaMK
PKA
PKC
Trk Receptor
Pathway
Anti-infection
Epigenetics
Neuronal Signaling
Protein Tyrosine Kinase/RTK
Stem Cell/Wnt
TGF-beta/Smad
Source data