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Compound Detail

CHEMBL4744811

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C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CC[C@H]1CC[C@H](NC(=O)c2cc3ccccc3[nH]2)CC1

Basic Information

ChEMBL ID CHEMBL4744811
Phase Preclinical
Structure Type MOL
InChI Key ADDKZOUNFAZVBP-DZNWXHPMSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

461.6
MW (Da)
4.29
ALogP
5
HBA
3
HBD
96.3
PSA (Ų)
0.51
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H35N5O2
MW 461.61
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.61

Activity Summary

Ki 5 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 7.68 7.675 21.0 2
D(2) dopamine receptor
CHEMBL217
Ki 7.06 7.02 86.2 2
Mu-type opioid receptor
CHEMBL233
Ki 4.66 4.66 21900.0 1

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