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Compound Detail

CHEMBL199931

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CN1CC[C@]23c4c5ccc(OC(=O)CCCCCCCCC(=O)Oc6ccc7c(c6)[C@@]68CCCCC6[C@@H](C7)N(CC6CCC6)CC8)c4O[C@H]2[C@@H](O)C=C[C@H]3[C@H]1C5

Basic Information

ChEMBL ID CHEMBL199931
Phase Preclinical
Structure Type MOL
InChI Key VAFOYDSKVKJZEN-OXGMEHGPSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

763.0
MW (Da)
7.98
ALogP
8
HBA
1
HBD
88.5
PSA (Ų)
0.10
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C48H62N2O6
MW 763.03
Aromatic Rings 2
Heavy Atoms 56
NP-Likeness 1.11

Activity Summary

Ki 3 meas. best 9.96
EC50 2 meas. best 8.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL237
Ki 9.96 9.96 0.1 1
Mu-type opioid receptor
CHEMBL233
Ki 9.66 9.66 0.2 1
Kappa-type opioid receptor
CHEMBL237
EC50 8.64 8.64 2.3 1
Mu-type opioid receptor
CHEMBL233
EC50 8.6 8.6 2.5 1
Delta-type opioid receptor
CHEMBL236
Ki 8.41 8.41 3.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16392810 10.1021/jm050577x Mu-type opioid receptor 6
16392810 10.1021/jm050577x Kappa-type opioid receptor 5
16392810 10.1021/jm050577x Delta-type opioid receptor 1
16392810 10.1021/jm050577x Opioid receptors; mu & kappa 1
16392810 10.1021/jm050577x Opioid receptors; delta & kappa 1

Data from ChEMBL 36 via Core Engine