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Compound Detail

CHEMBL369919

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O=C(CCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(C[C@@H]1CCCO1)CC3)Oc1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(C[C@@H]1CCCO1)CC3

Basic Information

ChEMBL ID CHEMBL369919
Phase Preclinical
Structure Type MOL
InChI Key XPVQMCQVPCFYJK-LHQHLCNUSA-N
3
Targets
6
Activities
3
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

821.2
MW (Da)
9.79
ALogP
8
HBA
0
HBD
77.5
PSA (Ų)
0.10
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C52H72N2O6
MW 821.16
Aromatic Rings 2
Heavy Atoms 60
NP-Likeness 0.31

Activity Summary

Ki 3 meas. best 9.17
EC50 2 meas. best 8.06
IC50 1 meas. best 6.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL233
Ki 9.17 9.17 0.7 1
Kappa-type opioid receptor
CHEMBL237
Ki 8.92 8.92 1.2 1
Delta-type opioid receptor
CHEMBL236
Ki 8.08 8.08 8.3 1
Kappa-type opioid receptor
CHEMBL237
EC50 8.06 8.06 8.8 1
Mu-type opioid receptor
CHEMBL233
EC50 7.92 7.92 12.0 1
Mu-type opioid receptor
CHEMBL233
IC50 6.44 6.44 360.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16392810 10.1021/jm050577x Mu-type opioid receptor 5
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