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Compound Detail

CHEMBL1427763

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CCN(CC)CCOC(=O)c1ccc(N/C=C(/C#N)c2nc(-c3ccc(OC)c(OC)c3)cs2)cc1

Basic Information

ChEMBL ID CHEMBL1427763
Phase Preclinical
Structure Type MOL
InChI Key VOMJABLLAXJBNQ-FXBPSFAMSA-N
8
Targets
12
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

506.6
MW (Da)
5.30
ALogP
9
HBA
1
HBD
96.7
PSA (Ų)
0.26
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H30N4O4S
MW 506.63
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.51

Activity Summary

IC50 11 meas. best 5.52
EC50 1 meas. best 4.87

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Ubiquitin-conjugating enzyme E2 N
CHEMBL6089
IC50 5.52 5.47 3016.0 2
Bcl-2-related protein A1
CHEMBL1293239
IC50 5.46 5.46 3440.0 1
Apoptotic protease-activating factor 1
CHEMBL1795093
IC50 5.41 5.4 3930.0 2
Unchecked
CHEMBL612545
IC50 5.38 5.38 4155.0 1
SUMO-activating enzyme
CHEMBL2095174
IC50 5.15 5.04 7120.0 2
Plectin
CHEMBL1293240
IC50 4.9 4.9 12500.0 1
Unchecked
CHEMBL612545
EC50 4.87 4.87 13500.0 1
26S proteasome non-ATPase regulatory subunit 14
CHEMBL2007629
IC50 4.63 4.63 23200.0 1
Prothrombin
CHEMBL4471
IC50 4.54 4.54 28700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Ubiquitin-conjugating enzyme E2 N IC50 = 3016.0 nM 5.52 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for the identification of U... -
Bcl-2-related protein A1 IC50 = 3440.0 nM 5.46 PUBCHEM_BIOASSAY: Dose Response confirmation of UBC13 Polyubiquitin Inhibitors u... -
Ubiquitin-conjugating enzyme E2 N IC50 = 3761.0 nM 5.42 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for the identification of U... -
Apoptotic protease-activating factor 1 IC50 = 3930.0 nM 5.41 PUBCHEM_BIOASSAY: SAR analysis of small molecule inhibitors of Apaf-1 in a Fluor... -
Apoptotic protease-activating factor 1 IC50 = 4090.0 nM 5.39 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 in a Fluore... -
Unchecked IC50 = 4155.0 nM 5.38 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Inhibitors of Mycobacterium... -
SUMO-activating enzyme IC50 = 7120.0 nM 5.15 PUBCHEM_BIOASSAY: AlphaScreen confirmatory assay for validation of inhibitors of... -
SUMO-activating enzyme IC50 = 11740.0 nM 4.93 PUBCHEM_BIOASSAY: uHTS HTRF assay for identification of inhibitors of SUMOylatio... -
Plectin IC50 = 12500.0 nM 4.9 PUBCHEM_BIOASSAY: uHTS identification of small molecule antagonists of the bindi... -
Unchecked EC50 = 13500.0 nM 4.87 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
26S proteasome non-ATPase regulatory subunit 14 IC50 = 23200.0 nM 4.63 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS RPN11 inhibitor hits in a F... -
Prothrombin IC50 = 28700.0 nM 4.54 PUBCHEM_BIOASSAY: Dose Response validation of uHTS RPN11 inhibitor hits using a ... -

Data from ChEMBL 36 via Core Engine