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Compound Detail

CHEMBL606960

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COc1ccc2c3c1O[C@H]1c4[nH]c5c(c4C[C@H]4[C@@H](C2)N(C)CC[C@]314)C[C@H]1[C@H]2Cc3ccc(OC)c4c3[C@@]1(CCN2C)[C@H]5O4

Basic Information

ChEMBL ID CHEMBL606960
Phase Preclinical
Structure Type MOL
InChI Key BOZJVDGQCWRTFI-NSHPJJRGSA-N
2
Targets
2
Activities
1
Assay Types
3
PK Parameters
5
Publications
0
Known Names

Molecular Properties

577.7
MW (Da)
4.64
ALogP
6
HBA
1
HBD
59.2
PSA (Ų)
0.48
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H39N3O4
MW 577.73
Aromatic Rings 3
Heavy Atoms 43
NP-Likeness 0.84

Activity Summary

IC50 2 meas. best 6.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Opioid receptor (mu and kappa)
CHEMBL2111465
IC50 6.48 6.48 330.0 1
Delta-type opioid receptor
CHEMBL3222
IC50 6.0 6.0 1000.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ke - - Cavia porcellus
Ke - - Cavia porcellus
Ke - - Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2832604 10.1021/jm00399a026 Opioid receptor (mu and kappa) 4
2832604 10.1021/jm00399a026 Delta-type opioid receptor 4
2832604 10.1021/jm00399a026 Unchecked 2
2832604 10.1021/jm00399a026 Kappa-type opioid receptor 1
2832604 10.1021/jm00399a026 Mu-type opioid receptor 1

Data from ChEMBL 36 via Core Engine