General
Preferred name
L-745870
Synonyms
L-745,870 hydrochloride ()
L-745,870 trihydrochloride ()
CHEMBL267014 ()
L 745,870 ()
L-745,870 ()
L-745870 (hydrochloride) ()
L-745870 trihydrochloride ()
L-745870 hydrochloride ()
L745870 ()
L-745,870 (hydrochloride) ()
P&D ID
PD047407
CAS
866021-03-6
158985-00-3
1173023-36-3
Tags
available
drug candidate
probe
Drug indication
Psychotic disorder
Probe info
Probe type
calculated probe
experimental probe
P&D approved
Probe selectivity
protein-selective
Probe sources
Chemical Probes.org
High-quality chemical probes
Tool Compound Set
Probe targets
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 L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and ¦Á-adrenoceptors[1][2][3].
PRICE 45
DESCRIPTION L-745870 hydrochloride has excellent brain penetration.?L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 receptor affinity with a Ki of 960 nM and D3 receptor affinity with a Ki of 2300 nM.?
PRICE 117
DESCRIPTION L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and ¦Á-adrenoceptors[1][2][3].
PRICE 70
DESCRIPTION L-745870 is an orally active, selective, and efficient dopamine D4 receptor antagonist that crosses the blood-brain barrier. It also inhibits D2 receptors, 5-HT2 receptors, and ??-adrenergic receptors, useful in neurological disease studies.
MOA Antagonist (Chemical Probes.org)
DESCRIPTION Selective D4 dopamine receptor antagonist (LOPAC library)
DESCRIPTION L-745870 hydrochloride has excellent brain penetration. L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 receptor affinity with a Ki of 960 nM and D3 receptor affinity with a Ki of 2300 nM.  (TargetMol Bioactive Compound Library)
DESCRIPTION High affinity D2 antagonist (Tocris Bioactive Compound Library)
DESCRIPTION Highly selective D4 antagonist (Tocriscreen Total)
DESCRIPTION L-745,870 trihydrochloride is the trihydrochloride salt of L-745,870, which is highly selective and potent D4 dopamine receptor antagonist with Ki value of 0.51nM. It is > 1000-fold selective over 5-HT2, D1 and D5 receptors. It has antipsychotic effects in animal models, but it was not effective in human trials. (BOC Sciences Bioactive Compounds)
DESCRIPTION L-745870 trihydrochloride is a highly potent and selective D4 dopamine receptor antagonist. (TargetMol Bioactive Compound Library)
DESCRIPTION L-745870 is an orally active, selective, and efficient dopamine D4 receptor antagonist that crosses the blood-brain barrier. It also inhibits D2 receptors, 5-HT2 receptors, and α-adrenergic receptors, useful in neurological disease studies. (TargetMol Bioactive Compound Library)
Cell lines
0
Organisms
2
Compound Sets
23
BOC Sciences Bioactive Compounds
l-745-870-trihydrochloride-cas-866021-03-6-item-169560
Cayman Chemical Bioactives
37586
Chemical Probes.org
l-745870
Concise Guide to Pharmacology 2017/18
3303
Concise Guide to Pharmacology 2019/20
3303
Concise Guide to Pharmacology 2021/22
3303
Concise Guide to Pharmacology 2023/24
3303
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
DMTGR25
DrugMatrix
Guide to Pharmacology
3303
High-quality chemical probes
PD047407
Ki Database
L 745,870
L-745870
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL267014
MedChem Express Bioactive Compound Library
HY-14325B
HY-14325
ReFrame library
TargetMol Bioactive Compound Library
T11799
T22904
T11799L
Tocris Bioactive Compound Library
1002
Tocriscreen Total
Tool Compound Set
ZINC Tool Compounds
ZINC000095803215
External IDs
45
Properties
(calculated by RDKit )
Molecular Weight
326.13
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
1
Rotatable Bonds
3
Ring Count
4
Aromatic Ring Count
3
cLogP
3.54
TPSA
35.16
Fraction CSP3
0.28
Chiral centers
0.0
Largest ring
6.0
QED
0.8
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Selectivity
D4
Target
Dopamine D4 receptor
5-HT2
D2
D3
Sigma Receptor
α-adrenergic receptor
human D2 receptor
human D3 receptor
human D4 receptor
DRD1, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR6, HTR7
Dopamine Receptor
DRD4
Primary Target
D4 Receptors
MOA
Antagonist
Dopamine Receptor antagonist
Pathway
GPCR/G protein
Neuroscience
Neuronal Signaling
Target class
GPCR
Target subclass
Dopamine receptor
Source data