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Compound Detail

CHEMBL4082150

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Cc1ccc(Sc2ccccc2N2CCN(CCc3c(C)nc4n(c3=O)CCCC4O)CC2)c(C)c1.Cl

Basic Information

ChEMBL ID CHEMBL4082150
Phase Preclinical
Structure Type MOL
InChI Key BVHJKISMBSDSFW-UHFFFAOYSA-N
Parent Compound CHEMBL4117087
Active Moiety CHEMBL4117087
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

504.7
MW (Da)
4.51
ALogP
7
HBA
1
HBD
61.6
PSA (Ų)
0.53
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H37ClN4O2S
MW 541.16
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.84

Activity Summary

IC50 2 meas. best 6.06
EC50 1 meas. best 5.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(2) dopamine receptor
CHEMBL217
IC50 6.06 6.06 875.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
EC50 5.96 5.96 1100.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
IC50 5.94 5.94 1160.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28774576 10.1016/j.bmc.2017.07.040 5-hydroxytryptamine receptor 1A 1
28774576 10.1016/j.bmc.2017.07.040 D(2) dopamine receptor 1
28774576 10.1016/j.bmc.2017.07.040 5-hydroxytryptamine receptor 2A 1

Data from ChEMBL 36 via Core Engine