General
Preferred name
Englerin-A
Synonyms
GTPL8372 ()
(-)-englerin A ()
ENGLERIN A ()
P&D ID
PD049360
CAS
1094250-15-3
Tags
available
drug candidate
probe
Drug indication
Discovery agent
Probe info
Probe type
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
1
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)
MOA
Agonist;Induces TRPC4/5-dependent calcium ion influx and cell death
COMMENT
Cytotoxicity was observed at 17 nM and 45 nM at different timepoints. Cell EC50s for TRPC4 and TRPC5 are 11 nM and 8 nM, respectively; therefore, there is an insufficient window between on-target activity and cytotoxicity to interpret cellular effects of the compound as target-based. Mar 13 2017 - 9:44am; There have been several papers showing that this compound activates TRPC4/5 including doi: 10.1002/anie.201411511. The data in those papers is quite convincing that the compound at low nM concentrations activates these channels and that it may mediate some of its anti-tumor activity via this effect. However, there is no convincing dataset regarding potential off-targets, as it has not yet been broadly screened against kinases, GPCRs, ion channels, and so on. Thus, provided the user does the appropriate controls (e.g., TRPC4/5 KO cells as a control), the compound will likely be useful. Mar 20 2017 - 8:33pm
DESCRIPTION
(-)-englerin A is a plant extract from the bark of Phyllanthus engleri . (-)-englerin A is a potent and selective agonist of TRPC4 and TRPC5 calcium channels with cytotoxic activity selective for several renal cancer cell lines . The (+) enantiomer is inactive against the same cells . The compound has been chemically synthesised .
(GtoPdb)
MOA
Agonist
(Chemical Probes.org)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
8
Organisms
0
Compound Sets
9
Chemical Probes.org
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
DrugMAP
Guide to Pharmacology
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
16
Molecular Weight
442.24
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
1
Rotatable Bonds
6
Ring Count
4
Aromatic Ring Count
1
cLogP
3.77
TPSA
82.06
Fraction CSP3
0.62
Chiral centers
7.0
Largest ring
6.0
QED
0.53
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Member status
member
MOA
TRPC4 gene stimulator
Target subclass
Transient receptor potential channels
Transient receptor potential channels, Transient receptor potential channels
Target class
Ion channel
Ion Channel, Ion Channel
Target
TRP Channel
TRPC4, TRPC5
Pathway
Membrane Transporter/Ion Channel
Neuronal Signaling
Control
(+)-englerin A
Source data
