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Compound Detail

CHEMBL1627314

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

Basic Information

ChEMBL ID CHEMBL1627314
Phase Preclinical
Structure Type MOL
InChI Key YRMKMEPMFOFXGH-UHFFFAOYSA-N
4
Targets
7
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

491.4
MW (Da)
3.79
ALogP
5
HBA
3
HBD
80.8
PSA (Ų)
0.45
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 C24H28Cl2N4O3
MW 491.42
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.16

Activity Summary

Ki 6 meas. best 9.04
IC50 1 meas. best 8.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 9.04 8.98 0.9 2
D(3) dopamine receptor
CHEMBL234
IC50 8.82 8.82 1.5 1
Unchecked
CHEMBL612545
Ki 6.94 6.625 115.0 2
D(2) dopamine receptor
CHEMBL217
Ki 6.66 6.66 217.0 1
D(4) dopamine receptor
CHEMBL219
Ki 5.69 5.69 2040.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19331412 10.1021/jm900095y Unchecked 6
19331412 10.1021/jm900095y D(3) dopamine receptor 3
19331412 10.1021/jm900095y D(4) dopamine receptor 1
19331412 10.1021/jm900095y D(1A) dopamine receptor 1
25826710 10.1021/jm501512b D(2) dopamine receptor 1
25826710 10.1021/jm501512b D(3) dopamine receptor 1
25826710 10.1021/jm501512b D(4) dopamine receptor 1
25826710 10.1021/jm501512b Unchecked 1
25826710 10.1021/jm501512b Dopamine receptors; D3 & D4 1

Data from ChEMBL 36 via Core Engine