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Compound Detail

CHEMBL4456754

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O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cncnc1

Basic Information

ChEMBL ID CHEMBL4456754
Phase Preclinical
Structure Type MOL
InChI Key ZZGIOJNVAOUXRN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

332.8
MW (Da)
1.29
ALogP
6
HBA
1
HBD
74.2
PSA (Ų)
0.91
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H17ClN6O
MW 332.80
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -2.81

Activity Summary

IC50 1 meas. best 4.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(2) dopamine receptor
CHEMBL217
IC50 4.14 4.14 72516.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
D(2) dopamine receptor IC50 = 72516.0 nM 4.14 Antagonist activity at human D2L receptor expressed in CHOK1 cells assessed as s... 30883109

Literature References

PubMed DOI Target Context # Activities
30883109 10.1021/acs.jmedchem.9b00231 D(2) dopamine receptor 9
30883109 10.1021/acs.jmedchem.9b00231 D(4) dopamine receptor 9
30883109 10.1021/acs.jmedchem.9b00231 D(3) dopamine receptor 5
30883109 10.1021/acs.jmedchem.9b00231 Unchecked 5
30883109 10.1021/acs.jmedchem.9b00231 Dopamine receptors; D3 & D4 1

Data from ChEMBL 36 via Core Engine