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Compound Detail

CHEMBL297756

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Cc1ccc(/C=C/C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5C3(CCN4CC3CC3)[C@H]2O6)cc1

Basic Information

ChEMBL ID CHEMBL297756
Phase Preclinical
Structure Type MOL
InChI Key JZKZQHCZPOYVJT-GPBMLUTFSA-N
4
Targets
6
Activities
2
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

486.6
MW (Da)
3.46
ALogP
5
HBA
3
HBD
82.0
PSA (Ų)
0.56
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H34N2O4
MW 486.61
Aromatic Rings 2
Heavy Atoms 36
NP-Likeness 0.99

Activity Summary

Ki 4 meas. best 9.64
IC50 2 meas. best 7.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL4354
Ki 9.64 9.64 0.2 1
Kappa-type opioid receptor
CHEMBL3952
Ki 9.22 7.995 0.6 2
Delta-type opioid receptor
CHEMBL236
Ki 8.02 8.02 9.6 1
Kappa-type opioid receptor
CHEMBL3952
IC50 7.9 7.9 12.6 1
Kappa-type opioid receptor
CHEMBL4329
IC50 4.77 4.77 17100.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ke 0.2 nM Cavia porcellus
Ke - - Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00583-F Kappa-type opioid receptor 4
- 10.1016/0960-894X(95)00583-F Mu-type opioid receptor 1
- 10.1016/0960-894X(95)00583-F Delta-type opioid receptor 1
- 10.1016/0960-894X(95)00583-F Cavia porcellus 1
- 10.1016/0960-894X(95)00583-F Mus musculus 1

Data from ChEMBL 36 via Core Engine