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Compound Detail

CHEMBL334715

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N=C(N)NCCC[C@@H](NC(=O)c1cccc2c3c([nH]c12)[C@@H]1Oc2c(O)ccc4c2C12CCN(CC1CC1)C(C4)[C@]2(O)C3)C(=O)O

Basic Information

ChEMBL ID CHEMBL334715
Phase Preclinical
Structure Type MOL
InChI Key SIUVQQDAATZZEL-YFMZUUBZSA-N
3
Targets
4
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

614.7
MW (Da)
2.02
ALogP
7
HBA
8
HBD
197.0
PSA (Ų)
0.10
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H38N6O6
MW 614.70
Aromatic Rings 3
Heavy Atoms 45
NP-Likeness 0.85

Activity Summary

Ki 4 meas. best 10.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL236
Ki 10.08 9.94 0.1 2
Kappa-type opioid receptor
CHEMBL3952
Ki 6.73 6.73 188.0 1
Mu-type opioid receptor
CHEMBL4354
Ki 6.48 6.48 333.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ke 3.3 nM -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7853332 10.1021/jm00003a002 Delta-type opioid receptor 5
7853332 10.1021/jm00003a002 Mu-type opioid receptor 2
7853332 10.1021/jm00003a002 Kappa-type opioid receptor 2
7853332 10.1021/jm00003a002 Opioid receptors; mu & delta 2
7853332 10.1021/jm00003a002 Opioid receptors; delta & kappa 2

Data from ChEMBL 36 via Core Engine