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Compound Detail

CHEMBL62601

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COc1c(-c2nc(CNC[C@@H]3CCN(Cc4ccccc4)C3)co2)cc(Br)c2ccccc12

Basic Information

ChEMBL ID CHEMBL62601
Phase Preclinical
Structure Type MOL
InChI Key DRRIHRQXXFYPBU-FQEVSTJZSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

506.4
MW (Da)
5.88
ALogP
5
HBA
1
HBD
50.5
PSA (Ų)
0.32
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H28BrN3O2
MW 506.44
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -0.99

Activity Summary

Ki 5 meas. best 5.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 5.23 5.23 5850.0 1
D(4) dopamine receptor
CHEMBL219
Ki 4.81 4.81 15500.0 1
D(2) dopamine receptor
CHEMBL217
Ki 4.76 4.55 17500.0 2
D(1A) dopamine receptor
CHEMBL2967
Ki 4.0 4.0 100000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10987445 10.1016/s0960-894x(00)00405-4 D(2) dopamine receptor 2
10987445 10.1016/s0960-894x(00)00405-4 D(1A) dopamine receptor 1
10987445 10.1016/s0960-894x(00)00405-4 D(3) dopamine receptor 1
10987445 10.1016/s0960-894x(00)00405-4 D(4) dopamine receptor 1

Data from ChEMBL 36 via Core Engine