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Compound Detail

CHEMBL5434650

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CCc1cc(Cl)c(OC)c(N2CCN(C[C@@H]3C[C@@H](O)CN3CCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1

Basic Information

ChEMBL ID CHEMBL5434650
Phase Preclinical
Structure Type MOL
InChI Key ACUOSRXKTFDQLE-IOWSJCHKSA-N
4
Targets
9
Activities
3
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

619.2
MW (Da)
4.93
ALogP
6
HBA
1
HBD
59.5
PSA (Ų)
0.33
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H47ClN4O3
MW 619.25
Aromatic Rings 3
Heavy Atoms 44
NP-Likeness -0.48

Activity Summary

EC50 5 meas. best 7.6
Ki 3 meas. best 6.96
IC50 1 meas. best 5.53

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
EC50 7.6 6.9067 25.1 3
D(3) dopamine receptor
CHEMBL234
Ki 6.96 6.96 111.0 1
Mu-type opioid receptor
CHEMBL233
Ki 6.42 6.42 377.0 1
D(2) dopamine receptor
CHEMBL217
Ki 6.06 6.06 870.0 1
D(3) dopamine receptor
CHEMBL234
IC50 5.53 5.53 2951.2 1
Mu-type opioid receptor
CHEMBL2858
EC50 5.48 5.48 3311.3 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
37467430 10.1021/acs.jmedchem.3c00417 Mu-type opioid receptor 8
37467430 10.1021/acs.jmedchem.3c00417 D(3) dopamine receptor 6
37467430 10.1021/acs.jmedchem.3c00417 D(2) dopamine receptor 1
37467430 10.1021/acs.jmedchem.3c00417 Unchecked 1

Data from ChEMBL 36 via Core Engine