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Compound Detail

CHEMBL416788

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Cc1cc(O)cc(C)c1C(NC(=O)C1Cc2ccccc2CN1)C(=O)O

Basic Information

ChEMBL ID CHEMBL416788
Phase Preclinical
Structure Type MOL
InChI Key ONMKFGZUBQSUFN-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

354.4
MW (Da)
1.97
ALogP
4
HBA
4
HBD
98.7
PSA (Ų)
0.67
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H22N2O4
MW 354.41
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness 0.29

Activity Summary

IC50 3 meas. best 8.8
Ki 2 meas. best 8.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL236
IC50 8.8 8.8 1.6 1
Delta-type opioid receptor
CHEMBL236
Ki 8.74 8.74 1.8 1
Mu-type opioid receptor
CHEMBL233
IC50 6.05 6.05 894.0 1
Mu-type opioid receptor
CHEMBL233
Ki 6.03 6.03 945.0 1
Kappa-type opioid receptor
CHEMBL237
IC50 4.43 4.43 37500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11448220 10.1021/jm015532k Delta-type opioid receptor 1
11448220 10.1021/jm015532k Mu-type opioid receptor 1
11448220 10.1021/jm015532k Kappa-type opioid receptor 1
12699761 10.1016/s0960-894x(03)00194-x Mu-type opioid receptor 1
12699761 10.1016/s0960-894x(03)00194-x Delta-type opioid receptor 1
12699761 10.1016/s0960-894x(03)00194-x Kappa-type opioid receptor 1

Data from ChEMBL 36 via Core Engine