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Compound Detail

CHEMBL4764883

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C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CC(O)CCNC(=O)c1cc2ccccc2[nH]1

Basic Information

ChEMBL ID CHEMBL4764883
Phase Preclinical
Structure Type MOL
InChI Key QVJKSJKBVZSPPJ-LMONUYQQSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

423.5
MW (Da)
2.09
ALogP
6
HBA
4
HBD
116.5
PSA (Ų)
0.46
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H29N5O3
MW 423.52
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.34

Activity Summary

Ki 5 meas. best 6.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 6.37 6.37 423.0 2
Mu-type opioid receptor
CHEMBL233
Ki 6.13 6.13 739.0 1
D(2) dopamine receptor
CHEMBL217
Ki 6.0 6.0 1010.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33062179 10.1021/acsmedchemlett.9b00660 D(1A) dopamine receptor 2
34699207 10.1021/acs.jmedchem.1c01433 D(2) dopamine receptor 2
34699207 10.1021/acs.jmedchem.1c01433 D(3) dopamine receptor 2
33062179 10.1021/acsmedchemlett.9b00660 D(2) dopamine receptor 1
33062179 10.1021/acsmedchemlett.9b00660 D(3) dopamine receptor 1
33062179 10.1021/acsmedchemlett.9b00660 Mu-type opioid receptor 1
34699207 10.1021/acs.jmedchem.1c01433 Unchecked 1

Data from ChEMBL 36 via Core Engine