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Compound Detail

CHEMBL3769612

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Cc1ccc(C)c(N2CCN(CC(O)CN3C(=O)NC(C)(c4ccc(F)cc4)C3=O)CC2)c1

Basic Information

ChEMBL ID CHEMBL3769612
Phase Preclinical
Structure Type MOL
InChI Key HKFCZKONZLVXFH-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

454.6
MW (Da)
2.39
ALogP
5
HBA
2
HBD
76.1
PSA (Ų)
0.66
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H31FN4O3
MW 454.55
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.64

Activity Summary

Ki 3 meas. best 7.25
IC50 1 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 7.25 7.25 56.0 1
5-hydroxytryptamine receptor 7
CHEMBL3155
IC50 6.0 6.0 1011.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 5.88 5.88 1304.0 1
D(2) dopamine receptor
CHEMBL217
Ki 5.74 5.74 1814.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26900658 10.1016/j.ejmech.2016.02.024 5-hydroxytryptamine receptor 7 3
26900658 10.1016/j.ejmech.2016.02.024 Unchecked 2
26900658 10.1016/j.ejmech.2016.02.024 5-hydroxytryptamine receptor 1A 1
26900658 10.1016/j.ejmech.2016.02.024 D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine