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Compound Detail

CHEMBL92917

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N=C(N)/N=C(\N)Nc1ccc2[nH]c3c(c2c1)C[C@@]1(O)C2Cc4ccc(O)c5c4[C@@]1(CCN2CC1CC1)[C@H]3O5

Basic Information

ChEMBL ID CHEMBL92917
Phase Preclinical
Structure Type MOL
InChI Key KAQDWUGWKGESIN-QNXFKXKFSA-N
3
Targets
3
Activities
1
Assay Types
3
PK Parameters
6
Publications
0
Known Names

Molecular Properties

513.6
MW (Da)
2.19
ALogP
5
HBA
7
HBD
169.0
PSA (Ų)
0.21
QED
2
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H31N7O3
MW 513.60
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness 0.85

Activity Summary

Ki 3 meas. best 9.65

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL3614
Ki 9.65 9.65 0.2 1
Mu-type opioid receptor
CHEMBL270
Ki 7.67 7.67 21.5 1
Delta-type opioid receptor
CHEMBL269
Ki 6.97 6.97 108.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ke 0.2 nM Cavia porcellus
Ke 14.0 nM Cavia porcellus
Ke - - -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10893314 10.1021/jm0000665 Kappa-type opioid receptor 3
10893314 10.1021/jm0000665 Mu-type opioid receptor 3
10893314 10.1021/jm0000665 Delta-type opioid receptor 3
10893314 10.1021/jm0000665 Unchecked 2
10893314 10.1021/jm0000665 Opioid receptors; mu & kappa 1
10893314 10.1021/jm0000665 Opioid receptors; delta & kappa 1

Data from ChEMBL 36 via Core Engine