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Compound Detail

CHEMBL435949

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COc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1

Basic Information

ChEMBL ID CHEMBL435949
Phase Preclinical
Structure Type MOL
InChI Key IDBBDQXTEVOOKW-UHFFFAOYSA-N
7
Targets
7
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

322.4
MW (Da)
2.89
ALogP
4
HBA
1
HBD
44.4
PSA (Ų)
0.80
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H22N4O
MW 322.41
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.47

Activity Summary

Ki 7 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(4) dopamine receptor
CHEMBL3361
Ki 8.85 8.85 1.4 1
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 6.99 6.99 102.8 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.39 6.39 405.6 1
D(2) dopamine receptor
CHEMBL339
Ki 6.36 6.36 438.0 1
D(3) dopamine receptor
CHEMBL3138
Ki 6.17 6.17 668.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 5.64 5.64 2311.6 1
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 5.13 5.13 7385.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11378358 10.1016/s0960-894x(01)00241-4 Muscarinic acetylcholine receptor M2 2
11378358 10.1016/s0960-894x(01)00241-4 5-hydroxytryptamine receptor 1D 1
11378358 10.1016/s0960-894x(01)00241-4 Glutamate NMDA receptor 1
11378358 10.1016/s0960-894x(01)00241-4 Glutamate [NMDA] receptor 1
11378358 10.1016/s0960-894x(01)00241-4 Histamine H1 receptor 1
11378358 10.1016/s0960-894x(01)00241-4 Mu-type opioid receptor 1
11378358 10.1016/s0960-894x(01)00241-4 Delta-type opioid receptor 1
11378358 10.1016/s0960-894x(01)00241-4 Kappa-type opioid receptor 1
11378358 10.1016/s0960-894x(01)00241-4 5-hydroxytryptamine receptor 5A 1
11378358 10.1016/s0960-894x(01)00241-4 5-hydroxytryptamine receptor 2C 1
11378358 10.1016/s0960-894x(01)00241-4 5-hydroxytryptamine receptor 1E 1
11378358 10.1016/s0960-894x(01)00241-4 D(4) dopamine receptor 1
11378358 10.1016/s0960-894x(01)00241-4 5-hydroxytryptamine receptor 1B 1
11378358 10.1016/s0960-894x(01)00241-4 D(1B) dopamine receptor 1
11378358 10.1016/s0960-894x(01)00241-4 D(1A) dopamine receptor 1
11378358 10.1016/s0960-894x(01)00241-4 5-hydroxytryptamine receptor 7 1
11378358 10.1016/s0960-894x(01)00241-4 5-hydroxytryptamine receptor 6 1
11378358 10.1016/s0960-894x(01)00241-4 5-hydroxytryptamine receptor 2A 1
11378358 10.1016/s0960-894x(01)00241-4 5-hydroxytryptamine receptor 1A 1
11378358 10.1016/s0960-894x(01)00241-4 D(3) dopamine receptor 1

Data from ChEMBL 36 via Core Engine