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Compound Detail

CHEMBL1311879

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Oc1c(N=Nc2ccccn2)ccc2ccccc12

Basic Information

ChEMBL ID CHEMBL1311879
Phase Preclinical
Structure Type MOL
InChI Key DKWJRBBUVAQOAC-UHFFFAOYSA-N
9
Targets
16
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

249.3
MW (Da)
4.36
ALogP
4
HBA
1
HBD
57.8
PSA (Ų)
0.69
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H11N3O
MW 249.27
Aromatic Rings 3
Heavy Atoms 19
NP-Likeness -0.58

Activity Summary

EC50 14 meas. best 5.59
IC50 2 meas. best 5.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL237
IC50 5.63 5.63 2320.0 1
Streptokinase A
CHEMBL1293228
EC50 5.59 5.59 2577.0 1
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.57 5.57 2666.0 1
BJ
CHEMBL614358
EC50 5.56 5.545 2763.0 4
Unchecked
CHEMBL612545
EC50 5.44 5.192 3594.0 5
Heat shock factor protein 1
CHEMBL5313
EC50 5.01 5.01 9825.0 1
Ephrin type-A receptor 4
CHEMBL1293259
IC50 4.86 4.86 13800.0 1
Beta-galactosidase
CHEMBL1293264
EC50 4.84 4.84 14500.0 1
Streptococcus
CHEMBL612313
EC50 4.6 4.6 25078.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Kappa-type opioid receptor IC50 = 2320.0 nM 5.63 PUBCHEM_BIOASSAY: uHTS identification of small molecule antagonists of the kappa... -
Streptokinase A EC50 = 2577.0 nM 5.59 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptococcus sp. 'group A' EC50 = 2666.0 nM 5.57 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
BJ EC50 = 2763.0 nM 5.56 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Comp... -
BJ EC50 = 2804.0 nM 5.55 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
BJ EC50 = 2840.0 nM 5.55 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Dose Response to Characterize Compound... -
BJ EC50 = 2991.0 nM 5.52 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked EC50 = 3594.0 nM 5.44 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked EC50 = 6465.0 nM 5.19 PUBCHEM_BIOASSAY: Luminescent Cell-Based Dose Titration Retest Counterscreen to ... -
Unchecked EC50 = 6460.0 nM 5.19 PUBCHEM_BIOASSAY: Dose response confirmation of small molecule activators of the... -
Unchecked EC50 = 7461.0 nM 5.13 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Unchecked EC50 = 9753.0 nM 5.01 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Heat shock factor protein 1 EC50 = 9825.0 nM 5.01 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Retest to Identify Potentiators o... -
Ephrin type-A receptor 4 IC50 = 13800.0 nM 4.86 PUBCHEM_BIOASSAY: Colorimetric assay for HTS discovery of chemical inhibitors of... -
Beta-galactosidase EC50 = 14500.0 nM 4.84 PUBCHEM_BIOASSAY: HTS Dose response counterscreen for assays utilizing the enzym... -
Streptococcus EC50 = 25078.0 nM 4.6 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -

Data from ChEMBL 36 via Core Engine