General
Preferred name
GR 113808
Synonyms
GR-113808 ()
[3H]GR 113808 ()
GR113808 ()
P&D ID
PD015324
CAS
144625-51-4
Tags
drug candidate
available
Drug indication
Discovery agent
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 GR 113808 is a potent and highly selective 5-HT4?receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors[1].
PRICE 120
DESCRIPTION GR 113808 is a selective 5-HT4 receptor antagonist that inhibits 5-HT1B, 5-HT2A, 5-HT2C, and 5-HT3 receptors, and attenuates dopamine release.
DESCRIPTION Potent, selective alpha2D antagonist (Tocris Bioactive Compound Library)
DESCRIPTION 5-HT4 serotonin receptor antagonist. (LOPAC library)
DESCRIPTION Potent, selective 5-HT4 antagonist (Tocriscreen Total)
DESCRIPTION GR 113808 is a potent and selective 5-HT4 receptor antagonist (pKB = 9.43 in human colonic muscle, Kd = 0.15 nM for binding to cloned human 5-HT4 receptors). GR 113808 displays > 300-fold selectivity for 5-HT4 over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors. (BOC Sciences Bioactive Compounds)
Cell lines
0
Organisms
2
Compound Sets
16
BOC Sciences Bioactive Compounds
gr-113808-cas-144625-51-4-item-77105
Cayman Chemical Bioactives
28733
Concise Guide to Pharmacology 2017/18
247
259
Concise Guide to Pharmacology 2019/20
247
259
Concise Guide to Pharmacology 2021/22
247
259
Concise Guide to Pharmacology 2023/24
247
259
Drug Repurposing Hub
DrugMAP
DMFU9VH
DrugMatrix
EUbOPEN Chemogenomics Library
EUB0000836
Guide to Pharmacology
247
259
Ki Database
GR 113808
LOPAC library
MedChem Express Bioactive Compound Library
HY-103152
Tocris Bioactive Compound Library
1322
Tocriscreen Total
External IDs
28
Properties
(calculated by RDKit )
Molecular Weight
393.17
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
1
Rotatable Bonds
7
Ring Count
3
Aromatic Ring Count
2
cLogP
1.6
TPSA
80.64
Fraction CSP3
0.53
Chiral centers
0.0
Largest ring
6.0
QED
0.72
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Selectivity
5-HT4
Primary Target
5-HT4 Receptors
MOA
Antagonist
serotonin receptor antagonist
Target
HTR4
5-HT Receptor
Pathway
GPCR/G protein
Neuronal Signaling
Recommended Cell Concentration
10 nM
Source data