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Compound Detail

CHEMBL1986418

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Oc1ccc2ccccc2c1/C=N/Nc1nnc(-c2ncc[nH]2)c2ccccc12

Basic Information

ChEMBL ID CHEMBL1986418
Phase Preclinical
Structure Type MOL
InChI Key QZBAXRCEGXLXOR-DHRITJCHSA-N
9
Targets
20
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

380.4
MW (Da)
4.32
ALogP
6
HBA
3
HBD
99.1
PSA (Ų)
0.32
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H16N6O
MW 380.41
Aromatic Rings 5
Heavy Atoms 29
NP-Likeness -1.00

Activity Summary

EC50 15 meas. best 6.75
IC50 5 meas. best 6.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 6.75 5.9271 178.0 7
ATP-dependent molecular chaperone HSP82
CHEMBL1293251
EC50 6.42 5.955 382.0 2
Unchecked
CHEMBL612545
IC50 6.28 6.28 520.0 1
Phospholipase A2
CHEMBL4426
IC50 5.82 5.715 1510.0 2
Streptokinase A
CHEMBL1293228
EC50 5.81 5.535 1554.0 2
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.7 5.7 1978.0 1
Zinc finger protein mex-5
CHEMBL1293319
EC50 5.61 5.61 2451.0 1
Cysteine protease ATG4B
CHEMBL1741221
IC50 5.6 5.435 2530.0 2
Streptococcus
CHEMBL612313
EC50 5.23 5.23 5844.0 1
RNA-binding protein pos-1
CHEMBL1293304
EC50 4.31 4.31 48713.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 178.0 nM 6.75 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Unchecked EC50 = 224.0 nM 6.65 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Unchecked EC50 = 292.0 nM 6.54 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
ATP-dependent molecular chaperone HSP82 EC50 = 382.0 nM 6.42 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay to Identify Inhibitors... -
Unchecked EC50 = 412.0 nM 6.38 PUBCHEM_BIOASSAY: Luminescence Cell-Based/Microorganism Dose Confirmation HTS to... -
Unchecked IC50 = 520.0 nM 6.28 PUBCHEM_BIOASSAY: Dose response counterscreen of uHTS chemical inhibitors of T-c... -
Unchecked EC50 = 714.0 nM 6.15 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Retest of Candida albicans Growth in t... -
Phospholipase A2 IC50 = 1510.0 nM 5.82 PUBCHEM_BIOASSAY: Dose response counterscreen of uHTS hits for ATG4B inhibitors ... -
Streptokinase A EC50 = 1554.0 nM 5.81 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptococcus sp. 'group A' EC50 = 1978.0 nM 5.7 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Zinc finger protein mex-5 EC50 = 2451.0 nM 5.61 PUBCHEM_BIOASSAY: Fluorescent Polarization Homogeneous Dose Response HTS to Iden... -
Phospholipase A2 IC50 = 2470.0 nM 5.61 PUBCHEM_BIOASSAY: Dose response counterscreen of uHTS hits for ATG4B inhibitors ... -
Cysteine protease ATG4B IC50 = 2530.0 nM 5.6 PUBCHEM_BIOASSAY: Dose response confirmation of the uHTS fluorescent assay for i... -
ATP-dependent molecular chaperone HSP82 EC50 = 3225.0 nM 5.49 PUBCHEM_BIOASSAY: Luminescence Cell-Based Secondary Assay to Identify Inhibitors... -
Cysteine protease ATG4B IC50 = 5400.0 nM 5.27 PUBCHEM_BIOASSAY: Dose response confirmation of the uHTS fluorescent assay for i... -
Streptokinase A EC50 = 5522.0 nM 5.26 PUBCHEM_BIOASSAY: Absorbance Microorganism-Based Dose Response HTS to Identify I... -
Streptococcus EC50 = 5844.0 nM 5.23 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Unchecked EC50 = 11413.0 nM 4.94 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay for toxicity in mammal... -
RNA-binding protein pos-1 EC50 = 48713.0 nM 4.31 PUBCHEM_BIOASSAY: Fluorescent Polarization Homogeneous Dose Response HTS to Iden... -
Unchecked EC50 = 82844.0 nM 4.08 PUBCHEM_BIOASSAY: Luminescence Cell-Based Confirmation at Dose to Identify Trans... -

Literature References

PubMed DOI Target Context # Activities
30523084 10.1126/science.aat9446 Plasmodium berghei 4
30523084 10.1126/science.aat9446 HepG2-CD81 2

Data from ChEMBL 36 via Core Engine