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Compound Detail

CHEMBL197796

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COc1ccc(NC(=O)N2CCN(c3ccc(SC)cc3)CC2)cc1N1CCN(C)CC1

Basic Information

ChEMBL ID CHEMBL197796
Phase Preclinical
Structure Type MOL
InChI Key BNXUKTBRYQQOIZ-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

455.6
MW (Da)
3.52
ALogP
6
HBA
1
HBD
51.3
PSA (Ų)
0.70
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H33N5O2S
MW 455.63
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.79

Activity Summary

Ki 5 meas. best 7.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1B
CHEMBL1898
Ki 7.78 7.78 16.7 1
5-hydroxytryptamine receptor 1D
CHEMBL1983
Ki 6.48 6.48 328.7 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.05 6.05 882.0 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 5.94 5.94 1145.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 5.88 5.88 1335.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16143528 10.1016/j.bmcl.2005.07.024 Muscarinic acetylcholine receptor M3 1
16143528 10.1016/j.bmcl.2005.07.024 D(2) dopamine receptor 1
16143528 10.1016/j.bmcl.2005.07.024 5-hydroxytryptamine receptor 7 1
16143528 10.1016/j.bmcl.2005.07.024 5-hydroxytryptamine receptor 6 1
16143528 10.1016/j.bmcl.2005.07.024 5-hydroxytryptamine receptor 2C 1
16143528 10.1016/j.bmcl.2005.07.024 5-hydroxytryptamine receptor 2A 1
16143528 10.1016/j.bmcl.2005.07.024 5-hydroxytryptamine receptor 1A 1
16143528 10.1016/j.bmcl.2005.07.024 Unchecked 1
16143528 10.1016/j.bmcl.2005.07.024 Muscarinic acetylcholine receptor M5 1
16143528 10.1016/j.bmcl.2005.07.024 Muscarinic acetylcholine receptor M4 1
16143528 10.1016/j.bmcl.2005.07.024 5-hydroxytryptamine receptor 1D 1
16143528 10.1016/j.bmcl.2005.07.024 5-hydroxytryptamine receptor 1B 1
16143528 10.1016/j.bmcl.2005.07.024 Muscarinic acetylcholine receptor M2 1
16143528 10.1016/j.bmcl.2005.07.024 Muscarinic acetylcholine receptor M1 1
16143528 10.1016/j.bmcl.2005.07.024 Histamine H1 receptor 1
16143528 10.1016/j.bmcl.2005.07.024 Mu-type opioid receptor 1
16143528 10.1016/j.bmcl.2005.07.024 Delta-type opioid receptor 1
16143528 10.1016/j.bmcl.2005.07.024 Kappa-type opioid receptor 1
16143528 10.1016/j.bmcl.2005.07.024 D(1B) dopamine receptor 1
16143528 10.1016/j.bmcl.2005.07.024 D(4) dopamine receptor 1

Data from ChEMBL 36 via Core Engine