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Compound Detail

CHEMBL4113058

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COc1ccc2c3c1O[C@H]1[C@@]4(OC)CC[C@@]5(C[C@@H]4CNCc4ccccc4)[C@@H](C2)N(CC2CC2)CC[C@]315

Basic Information

ChEMBL ID CHEMBL4113058
Phase Preclinical
Structure Type MOL
InChI Key PGANIOBIXBHMAK-BUVWRSTLSA-N
4
Targets
8
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

500.7
MW (Da)
4.71
ALogP
5
HBA
1
HBD
43.0
PSA (Ų)
0.57
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H40N2O3
MW 500.68
Aromatic Rings 2
Heavy Atoms 37
NP-Likeness 0.93

Activity Summary

EC50 4 meas. best 8.07
Ki 4 meas. best 10.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL237
Ki 10.4 10.4 0.0 1
Kappa-type opioid receptor
CHEMBL237
EC50 8.07 8.07 8.4 1
Mu-type opioid receptor
CHEMBL233
Ki 8.04 8.04 9.0 1
Mu-type opioid receptor
CHEMBL233
EC50 7.3 7.3 50.4 1
Opioid growth factor receptor-like protein 1
CHEMBL3638334
Ki 6.83 6.83 147.0 1
Delta-type opioid receptor
CHEMBL236
Ki 6.31 6.31 493.6 1
Delta-type opioid receptor
CHEMBL236
EC50 6.28 6.28 526.0 1
Opioid growth factor receptor-like protein 1
CHEMBL3638334
EC50 5.91 5.91 1224.7 1

Activity Data Samples

Top measurements by pChEMBL value

Data from ChEMBL 36 via Core Engine