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Compound Detail

CHEMBL1541834

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Oc1c(CN2CCc3ccccc3C2)cc(Cl)c2cccnc12

Basic Information

ChEMBL ID CHEMBL1541834
Phase Preclinical
Structure Type MOL
InChI Key GINDUKKWVPOXHU-UHFFFAOYSA-N
10
Targets
24
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

324.8
MW (Da)
4.15
ALogP
3
HBA
1
HBD
36.4
PSA (Ų)
0.77
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 C19H17ClN2O
MW 324.81
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.05

Activity Summary

EC50 16 meas. best 6.15
IC50 8 meas. best 6.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MES-SA/Dx5
CHEMBL613827
IC50 6.57 6.275 270.0 2
Unchecked
CHEMBL612545
EC50 6.15 5.5583 712.0 6
ATP-dependent molecular chaperone HSP82
CHEMBL1293251
EC50 6.07 5.695 849.0 2
MES-SA
CHEMBL614343
IC50 5.74 5.725 1810.0 2
Streptokinase A
CHEMBL1293228
EC50 5.67 5.67 2153.0 1
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.53 5.53 2948.0 1
Nucleic Acid
CHEMBL345
EC50 5.24 5.24 5810.0 1
Unchecked
CHEMBL612545
IC50 5.13 4.9175 7360.0 4
BJ
CHEMBL614358
EC50 5.07 5.0333 8454.0 3
Streptococcus
CHEMBL612313
EC50 5.03 5.03 9326.0 1
HT-1080
CHEMBL614580
EC50 4.65 4.65 22200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MES-SA/Dx5 IC50 = 270.0 nM 6.57 Cytotoxicity against multidrug resistance human MES-SA/Dx5 cells assessed as cel... 35613553
Unchecked EC50 = 712.0 nM 6.15 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Retest of Candida albicans Growth in t... -
ATP-dependent molecular chaperone HSP82 EC50 = 849.0 nM 6.07 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay to Identify Inhibitors... -
Unchecked EC50 = 973.0 nM 6.01 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
Unchecked EC50 = 1032.0 nM 5.99 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
MES-SA/Dx5 IC50 = 1050.0 nM 5.98 Cytotoxicity against multidrug resistance human MES-SA/Dx5 cells assessed as cel... 35613553
MES-SA IC50 = 1810.0 nM 5.74 Cytotoxicity against human MES-SA cells assessed as cell growth inhibition incub... 35613553
MES-SA IC50 = 1960.0 nM 5.71 Cytotoxicity against human MES-SA cells assessed as cell growth inhibition incub... 35613553
Streptokinase A EC50 = 2153.0 nM 5.67 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptococcus sp. 'group A' EC50 = 2948.0 nM 5.53 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
ATP-dependent molecular chaperone HSP82 EC50 = 4840.0 nM 5.32 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay to Measure Toxicity of... -
Nucleic Acid EC50 = 5810.0 nM 5.24 PUBCHEM_BIOASSAY: Luminescent HTS for small molecule inhibitors of MT1-MMP trans... -
Unchecked EC50 = 6006.0 nM 5.22 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked IC50 = 7360.0 nM 5.13 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -
Unchecked IC50 = 7646.0 nM 5.12 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Inhibitors of Mycobacterium... -
BJ EC50 = 8454.0 nM 5.07 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
BJ EC50 = 8601.0 nM 5.07 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked EC50 = 8710.0 nM 5.06 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Streptococcus EC50 = 9326.0 nM 5.03 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
BJ EC50 = 10861.0 nM 4.96 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Comp... -

Literature References

PubMed DOI Target Context # Activities
35613553 10.1021/acs.jmedchem.2c00076 MES-SA 2
35613553 10.1021/acs.jmedchem.2c00076 Unchecked 2
35613553 10.1021/acs.jmedchem.2c00076 MES-SA/Dx5 2

Data from ChEMBL 36 via Core Engine