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Compound Detail

CHEMBL599977

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CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(NC(=O)Nc4c(Cl)cccc4Cl)cc3CC[C@@H]21

Basic Information

ChEMBL ID CHEMBL599977
Phase Preclinical
Structure Type MOL
InChI Key DBFSWXFALPMOGP-LADGPHEKSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

516.9
MW (Da)
6.93
ALogP
3
HBA
3
HBD
64.6
PSA (Ų)
0.35
QED
2
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H24Cl3N3O2
MW 516.86
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.35

Activity Summary

Ki 2 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(1A) dopamine receptor
CHEMBL2056
Ki 9.15 9.15 0.7 1
D(2) dopamine receptor
CHEMBL217
Ki 5.96 5.96 1093.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
D(1A) dopamine receptor Ki = 0.7 nM 9.15 Binding affinity to dopamine D1 receptor 20061148
D(2) dopamine receptor Ki = 1093.0 nM 5.96 Binding affinity to dopamine D2 receptor 20061148

Literature References

PubMed DOI Target Context # Activities
20061148 10.1016/j.bmcl.2009.12.100 D(1A) dopamine receptor 1
20061148 10.1016/j.bmcl.2009.12.100 D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine