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Compound Detail

CHEMBL1774541

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COc1ccc2[nH]c(C(=O)NCCC(F)CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2c1

Basic Information

ChEMBL ID CHEMBL1774541
Phase Preclinical
Structure Type MOL
InChI Key WBGWXELVCBHOMZ-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

493.4
MW (Da)
4.76
ALogP
4
HBA
2
HBD
60.6
PSA (Ų)
0.48
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H27Cl2FN4O2
MW 493.41
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.36

Activity Summary

Ki 3 meas. best 8.82
IC50 1 meas. best 6.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 8.82 8.82 1.5 1
D(2) dopamine receptor
CHEMBL217
Ki 6.64 6.64 230.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.57 6.57 272.0 1
D(3) dopamine receptor
CHEMBL234
IC50 6.5 6.5 320.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21495689 10.1021/jm200288r D(3) dopamine receptor 3
21495689 10.1021/jm200288r D(2) dopamine receptor 2
21495689 10.1021/jm200288r 5-hydroxytryptamine receptor 1A 2
21495689 10.1021/jm200288r 5-hydroxytryptamine receptor 2A 1
21495689 10.1021/jm200288r D(4) dopamine receptor 1
21495689 10.1021/jm200288r Unchecked 1

Data from ChEMBL 36 via Core Engine