General
Preferred name
Pico145
Synonyms
HC-608 ()
Zerencotrep ()
P&D ID
PD098120
CAS
1628287-16-0
Tags
available
drug candidate
Drug Status
investigational
Max Phase
2.0
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 Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (-)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8[1].
PRICE 258
DESCRIPTION Pico145 is a potent, selective, and subtype-specific small-molecule inhibitor of TRPC1/4/5 channels . It competitively inhibits -induced TRPC5 activation . (GtoPdb)
DESCRIPTION Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, specifically inhibiting ( )-englerin A-activated TRPC4/TRPC5 channels with IC50s of 0.349 and 1.3 nM in cells, while showing no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, or TRPM8. (TargetMol Bioactive Compound Library)
Compound Sets
10
AdooQ Bioactive Compound Library
A13344
ChEMBL Drugs
CHEMBL4466522
Concise Guide to Pharmacology 2019/20
10291
Concise Guide to Pharmacology 2021/22
10291
Concise Guide to Pharmacology 2023/24
10291
CZ-OPENSCREEN Bioactive Library
EUbOPEN Chemogenomics Library
EUB0002038
Guide to Pharmacology
10291
MedChem Express Bioactive Compound Library
HY-101507
TargetMol Bioactive Compound Library
T16532
External IDs
9
Properties
(calculated by RDKit )
Molecular Weight
524.11
Hydrogen Bond Acceptors
9
Hydrogen Bond Donors
1
Rotatable Bonds
8
Ring Count
4
Aromatic Ring Count
4
cLogP
3.67
TPSA
100.51
Fraction CSP3
0.26
Chiral centers
0.0
Largest ring
6.0
QED
0.38
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
TRP Channel
TRPC4
TRPC4-TRPC1
TRPC5
TRPC5-TRPC1
Pathway
Membrane Transporter/Ion Channel
Neuronal Signaling
Recommended Cell Concentration
10 uM
Source data