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Compound Detail

CHEMBL510976

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Cc1cc(O)cc(C)c1C[C@H](C)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)O)C(C)(C)SSC1(C)C

Basic Information

ChEMBL ID CHEMBL510976
Phase Preclinical
Structure Type MOL
InChI Key XANRDWIUBJEDGB-LMSMQYTJSA-N
3
Targets
3
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

838.0
MW (Da)
3.90
ALogP
9
HBA
7
HBD
203.0
PSA (Ų)
0.14
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C42H52FN5O8S2
MW 838.04
Aromatic Rings 3
Heavy Atoms 58
NP-Likeness 0.57

Activity Summary

Ki 3 meas. best 8.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL269
Ki 8.63 8.63 2.3 1
Mu-type opioid receptor
CHEMBL270
Ki 6.39 6.39 406.0 1
Kappa-type opioid receptor
CHEMBL3952
Ki 5.43 5.43 3710.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ke 668.0 nM Cavia porcellus
Ke 4370.0 nM Cavia porcellus
Ke 0.785 nM Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18800771 10.1021/jm8004702 Mu-type opioid receptor 2
18800771 10.1021/jm8004702 Kappa-type opioid receptor 2
18800771 10.1021/jm8004702 Delta-type opioid receptor 2

Data from ChEMBL 36 via Core Engine