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Compound Detail

CHEMBL1460004

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COc1ccc(OCc2n(CC(=O)OC3CC(C)CCC3C(C)C)c3ccccc3[n+]2C)cc1.[Cl-]

Basic Information

ChEMBL ID CHEMBL1460004
Phase Preclinical
Structure Type MOL
InChI Key XBTSSWGMHQSDTR-UHFFFAOYSA-M
Parent Compound CHEMBL1621655
Active Moiety CHEMBL1621655
5
Targets
15
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

465.6
MW (Da)
5.06
ALogP
5
HBA
0
HBD
53.6
PSA (Ų)
0.34
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 C28H37ClN2O4
MW 501.07
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness 0.04

Activity Summary

IC50 12 meas. best 5.48
EC50 3 meas. best 5.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 5.8 5.795 1600.0 2
Unchecked
CHEMBL612545
IC50 5.48 4.5243 3338.0 7
Orexin/Hypocretin receptor type 1
CHEMBL5113
IC50 5.06 4.63 8686.0 2
X-box-binding protein 1
CHEMBL1741176
IC50 5.0 5.0 10000.0 1
Insulin-degrading enzyme
CHEMBL1293287
EC50 4.81 4.81 15541.0 1
HEK293
CHEMBL614818
IC50 4.77 4.77 17039.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 1600.0 nM 5.8 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Unchecked EC50 = 1630.0 nM 5.79 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Unchecked IC50 = 3338.0 nM 5.48 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Inhibitors of Mycobacterium... -
Orexin/Hypocretin receptor type 1 IC50 = 8686.0 nM 5.06 PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response as... -
X-box-binding protein 1 IC50 = 10000.0 nM 5.0 PUBCHEM_BIOASSAY: XBP1 DR counterscreen for CHOP. (Class of assay: confirmatory)... -
Unchecked IC50 = 15309.0 nM 4.82 PUBCHEM_BIOASSAY: Counterscreen for antagonists of the orexin 1 receptor (OX1R; ... -
Insulin-degrading enzyme EC50 = 15541.0 nM 4.81 PUBCHEM_BIOASSAY: Fluorescence polarization-based cell-based high throughput dos... -
HEK293 IC50 = 17039.0 nM 4.77 PUBCHEM_BIOASSAY: Counterscreen for activators of insulin-degrading enzyme (IDE)... -
Unchecked IC50 = 36630.0 nM 4.44 PUBCHEM_BIOASSAY: A counter screen for small molecule screen for inhibitors of t... -
Unchecked IC50 = 39640.0 nM 4.4 PUBCHEM_BIOASSAY: A Counter Screen to identiry small molecule screen for inhibit... -
Unchecked IC50 = 48890.0 nM 4.31 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -
Orexin/Hypocretin receptor type 1 IC50 = 63052.0 nM 4.2 PUBCHEM_BIOASSAY: Homogeneous Time Resolved Fluorescence (HTRF)-based cell-based... -
Unchecked IC50 = 74870.0 nM 4.13 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -
Unchecked IC50 = 80588.0 nM 4.09 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -

Data from ChEMBL 36 via Core Engine