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Compound Detail

CHEMBL3198912

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O=C(N/N=C/c1cc2c3c(c1O)CCCN3CCC2)c1ccccc1O

Basic Information

ChEMBL ID CHEMBL3198912
Phase Preclinical
Structure Type MOL
InChI Key XRPDZGHUTLBFJI-CIAFOILYSA-N
7
Targets
19
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

351.4
MW (Da)
2.56
ALogP
5
HBA
3
HBD
85.2
PSA (Ų)
0.59
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H21N3O3
MW 351.41
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.13

Activity Summary

EC50 16 meas. best 6.99
IC50 3 meas. best 4.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 6.99 5.935 102.0 8
ATP-dependent molecular chaperone HSP82
CHEMBL1293251
EC50 6.05 5.4867 895.0 3
Streptokinase A
CHEMBL1293228
EC50 5.15 5.15 7140.0 1
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.09 5.09 8164.0 1
Streptococcus
CHEMBL612313
EC50 4.92 4.92 12020.0 1
Serine/threonine-protein phosphatase
CHEMBL1293271
EC50 4.74 4.74 18232.0 1
BJ
CHEMBL614358
EC50 4.65 4.65 22400.0 1
Unchecked
CHEMBL612545
IC50 4.02 4.02 95290.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 102.0 nM 6.99 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Unchecked EC50 = 429.0 nM 6.37 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Retest of Candida albicans Growth in t... -
Unchecked EC50 = 558.0 nM 6.25 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response to Identify Inhibitors o... -
Unchecked EC50 = 687.0 nM 6.16 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response to Identify Inhibitors o... -
Unchecked EC50 = 798.0 nM 6.1 PUBCHEM_BIOASSAY: Luminescence Cell-Based HTS Dose Confirmation to Identify Inhi... -
ATP-dependent molecular chaperone HSP82 EC50 = 895.0 nM 6.05 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay to Identify Inhibitors... -
ATP-dependent molecular chaperone HSP82 EC50 = 2145.0 nM 5.67 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay to Measure Toxicity of... -
Unchecked EC50 = 2887.0 nM 5.54 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Unchecked EC50 = 3560.0 nM 5.45 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Streptokinase A EC50 = 7140.0 nM 5.15 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptococcus sp. 'group A' EC50 = 8164.0 nM 5.09 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptococcus EC50 = 12020.0 nM 4.92 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
ATP-dependent molecular chaperone HSP82 EC50 = 18054.0 nM 4.74 PUBCHEM_BIOASSAY: Luminescence Cell-Based Secondary Assay to Identify Inhibitors... -
Serine/threonine-protein phosphatase EC50 = 18232.0 nM 4.74 PUBCHEM_BIOASSAY: Luminescence Cell-Based Secondary Assay to Identify Inhibitors... -
BJ EC50 = 22400.0 nM 4.65 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Dose Response to Characterize Compound... -
Unchecked EC50 = 23735.0 nM 4.62 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay for toxicity in mammal... -
Unchecked IC50 = 95290.0 nM 4.02 PUBCHEM_BIOASSAY: A Counter Screen to identiry small molecule screen for inhibit... -

Data from ChEMBL 36 via Core Engine