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Compound Detail

CHEMBL1995152

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N=C(N)N/N=C/c1ccc(N(c2ccccc2)c2ccccc2)cc1.O=[N+]([O-])O

Basic Information

ChEMBL ID CHEMBL1995152
Phase Preclinical
Structure Type MOL
InChI Key DLIYPYGOQBSDLZ-BUGNPGDCSA-N
Parent Compound CHEMBL2010551
Active Moiety CHEMBL2010551
10
Targets
17
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

329.4
MW (Da)
3.97
ALogP
3
HBA
3
HBD
77.5
PSA (Ų)
0.38
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H20N6O3
MW 392.42
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -0.98

Activity Summary

IC50 10 meas. best 5.95
EC50 7 meas. best 5.69

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Ubiquitin-conjugating enzyme E2 N
CHEMBL6089
IC50 5.95 5.515 1114.0 2
Streptokinase A
CHEMBL1293228
EC50 5.69 5.69 2060.0 1
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.62 5.62 2391.0 1
Streptococcus
CHEMBL612313
EC50 5.47 5.47 3388.0 1
Bcl-2-related protein A1
CHEMBL1293239
IC50 5.42 5.42 3850.0 1
Unchecked
CHEMBL612545
EC50 5.29 5.0125 5124.0 4
Unchecked
CHEMBL612545
IC50 5.01 4.81 9860.0 3
26S proteasome non-ATPase regulatory subunit 14
CHEMBL2007629
IC50 4.75 4.75 18000.0 1
Apoptotic protease-activating factor 1
CHEMBL1795093
IC50 4.55 4.55 28200.0 1
Prothrombin
CHEMBL4471
IC50 4.38 4.38 41800.0 1
72 kDa type IV collagenase
CHEMBL333
IC50 4.18 4.18 66300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Ubiquitin-conjugating enzyme E2 N IC50 = 1114.0 nM 5.95 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for the identification of U... -
Streptokinase A EC50 = 2060.0 nM 5.69 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptococcus sp. 'group A' EC50 = 2391.0 nM 5.62 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptococcus EC50 = 3388.0 nM 5.47 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Bcl-2-related protein A1 IC50 = 3850.0 nM 5.42 PUBCHEM_BIOASSAY: Dose Response confirmation of UBC13 Polyubiquitin Inhibitors u... -
Unchecked EC50 = 5124.0 nM 5.29 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Retest of Candida albicans Growth in t... -
Ubiquitin-conjugating enzyme E2 N IC50 = 8239.0 nM 5.08 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for the identification of U... -
Unchecked EC50 = 8887.0 nM 5.05 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Unchecked IC50 = 9860.0 nM 5.01 PUBCHEM_BIOASSAY: A High Throughput Confirmatory Assay used to Identify Novel Co... -
Unchecked EC50 = 10369.0 nM 4.98 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Unchecked IC50 = 10910.0 nM 4.96 PUBCHEM_BIOASSAY: High Throughput Screening Assay used to Identify Novel Compoun... -
26S proteasome non-ATPase regulatory subunit 14 IC50 = 18000.0 nM 4.75 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS RPN11 inhibitor hits in a F... -
Unchecked EC50 = 18470.0 nM 4.73 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay for toxicity in mammal... -
Apoptotic protease-activating factor 1 IC50 = 28200.0 nM 4.55 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 in a Fluore... -
Unchecked IC50 = 34600.0 nM 4.46 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 using a LZ-... -
Prothrombin IC50 = 41800.0 nM 4.38 PUBCHEM_BIOASSAY: Dose Response validation of uHTS RPN11 inhibitor hits using a ... -
72 kDa type IV collagenase IC50 = 66300.0 nM 4.18 PUBCHEM_BIOASSAY: Dose Response validation of uHTS RPN11 inhibitor hits using a ... -

Data from ChEMBL 36 via Core Engine