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Compound Detail

CHEMBL3916122

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COc1ccc2c3c1O[C@H]1[C@@]4(OC)CC[C@@]5(C[C@@H]4COCc4ccccc4)[C@@H](C2)N(CC2CC2)CC[C@]315

Basic Information

ChEMBL ID CHEMBL3916122
Phase Preclinical
Structure Type MOL
InChI Key JHEVLALGAHRXET-BUVWRSTLSA-N
4
Targets
14
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

501.7
MW (Da)
5.14
ALogP
5
HBA
0
HBD
40.2
PSA (Ų)
0.50
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H39NO4
MW 501.67
Aromatic Rings 2
Heavy Atoms 37
NP-Likeness 0.95

Activity Summary

Ki 10 meas. best 10.05
EC50 4 meas. best 8.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL237
Ki 10.05 9.985 0.1 2
Mu-type opioid receptor
CHEMBL233
Ki 9.92 8.87 0.1 4
Kappa-type opioid receptor
CHEMBL237
EC50 8.37 8.37 4.3 1
Delta-type opioid receptor
CHEMBL236
Ki 8.04 7.93 9.2 2
Mu-type opioid receptor
CHEMBL233
EC50 7.97 7.97 10.8 1
Delta-type opioid receptor
CHEMBL236
EC50 7.83 7.83 14.7 1
Opioid growth factor receptor-like protein 1
CHEMBL3638334
Ki 6.27 6.17 532.0 2
Opioid growth factor receptor-like protein 1
CHEMBL3638334
EC50 5.79 5.79 1642.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Kappa-type opioid receptor Ki = 0.09 nM 10.05 Radioligand Dose-Displacement Binding Assay: Radioligand dose displacement assay... -
Mu-type opioid receptor Ki = 0.12 nM 9.92 Binding Assay: Binding assay of certain compounds of this invention to the opioi... -
Kappa-type opioid receptor Ki = 0.12 nM 9.92 Binding Assay: Binding assay of certain compounds of this invention to the opioi... -
Mu-type opioid receptor Ki = 1.52 nM 8.82 Radioligand Dose-Displacement Binding Assay: Radioligand dose-displacement bindi... -
Mu-type opioid receptor Ki = 2.0 nM 8.7 Binding Assay: Binding assay of certain compounds of this invention to the opioi... -
Kappa-type opioid receptor EC50 = 4.27 nM 8.37 Functional Assay: Functional [35S]GTPgammaS binding assays were conducted as fol... -
Mu-type opioid receptor Ki = 9.2 nM 8.04 Binding Assay: Binding assay of certain compounds of this invention to the opioi... -
Delta-type opioid receptor Ki = 9.2 nM 8.04 Binding Assay: Binding assay of certain compounds of this invention to the opioi... -
Mu-type opioid receptor EC50 = 10.78 nM 7.97 Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly ... -
Delta-type opioid receptor EC50 = 14.69 nM 7.83 Functional Assay: Functional [35S]GTPgammaS binding assays were conducted as fol... -
Delta-type opioid receptor Ki = 15.01 nM 7.82 Radioligand Dose-Displacement Binding Assay: Delta-opioid Receptor Binding Assay... -
Opioid growth factor receptor-like protein 1 Ki = 532.0 nM 6.27 Binding Assay: Binding assay of certain compounds of this invention to the opioi... -
Opioid growth factor receptor-like protein 1 Ki = 859.27 nM 6.07 Radioligand Dose-Displacement Binding Assay: Radioligand binding assays (screeni... -
Opioid growth factor receptor-like protein 1 EC50 = 1642.4 nM 5.79 Functional Assay: Functional [35S]GTPgammaS binding assays were conducted as fol... -

Data from ChEMBL 36 via Core Engine