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Compound Detail

CHEMBL599135

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CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/OCc4ccccc4)c3CC[C@@H]21

Basic Information

ChEMBL ID CHEMBL599135
Phase Preclinical
Structure Type MOL
InChI Key YUNGHULYKDVTOC-JJQUOXMWSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

447.0
MW (Da)
5.53
ALogP
4
HBA
1
HBD
45.1
PSA (Ų)
0.42
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H27ClN2O2
MW 446.98
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness 0.18

Activity Summary

Ki 4 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(1A) dopamine receptor
CHEMBL2056
Ki 9.7 9.7 0.2 1
D(1B) dopamine receptor
CHEMBL1850
Ki 8.6 8.6 2.5 1
D(2) dopamine receptor
CHEMBL217
Ki 7.16 7.16 69.0 1
D(4) dopamine receptor
CHEMBL219
Ki 5.08 5.08 8344.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20064718 10.1016/j.bmcl.2009.12.094 D(1A) dopamine receptor 1
20064718 10.1016/j.bmcl.2009.12.094 D(1B) dopamine receptor 1
20064718 10.1016/j.bmcl.2009.12.094 D(2) dopamine receptor 1
20064718 10.1016/j.bmcl.2009.12.094 D(4) dopamine receptor 1

Data from ChEMBL 36 via Core Engine