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Compound Detail

CHEMBL1487639

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O=Cc1ccc(O)c2ncccc12

Basic Information

ChEMBL ID CHEMBL1487639
Phase Preclinical
Structure Type MOL
InChI Key LIADJWREMDHKHQ-UHFFFAOYSA-N
6
Targets
19
Activities
2
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

173.2
MW (Da)
1.75
ALogP
3
HBA
1
HBD
50.2
PSA (Ų)
0.67
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C10H7NO2
MW 173.17
Aromatic Rings 2
Heavy Atoms 13
NP-Likeness 0.14

Activity Summary

EC50 13 meas. best 6.55
IC50 6 meas. best 6.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
BJ
CHEMBL614358
EC50 6.55 5.2625 284.0 4
Unchecked
CHEMBL612545
EC50 6.48 5.292 333.0 5
Unchecked
CHEMBL612545
IC50 6.42 5.4175 378.0 4
ATP-dependent molecular chaperone HSP82
CHEMBL1293251
EC50 5.84 5.3333 1449.0 3
Serine/threonine-protein phosphatase
CHEMBL1293271
EC50 5.41 5.41 3925.0 1
Indoleamine 2,3-dioxygenase 1
CHEMBL4685
IC50 5.36 5.36 4370.0 1
Catechol O-methyltransferase
CHEMBL2372
IC50 4.23 4.23 58884.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
BJ EC50 = 284.0 nM 6.55 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Dose Response to Characterize Compound... -
Unchecked EC50 = 333.0 nM 6.48 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Retest of Candida albicans Growth in t... -
Unchecked IC50 = 378.0 nM 6.42 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Inhibitors of Mycobacterium... -
ATP-dependent molecular chaperone HSP82 EC50 = 1449.0 nM 5.84 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay to Identify Inhibitors... -
Unchecked EC50 = 3790.0 nM 5.42 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Serine/threonine-protein phosphatase EC50 = 3925.0 nM 5.41 PUBCHEM_BIOASSAY: Luminescence Cell-Based Secondary Assay to Identify Inhibitors... -
Indoleamine 2,3-dioxygenase 1 IC50 = 4370.0 nM 5.36 Inhibition of recombinant human IDO1 expressed in Escherichia coli EC538 assesse... 33901770
BJ EC50 = 4432.0 nM 5.35 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
ATP-dependent molecular chaperone HSP82 EC50 = 6244.0 nM 5.21 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay to Measure Toxicity of... -
Unchecked IC50 = 6780.0 nM 5.17 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -
Unchecked IC50 = 8120.0 nM 5.09 PUBCHEM_BIOASSAY: A Counter Screen to identiry small molecule screen for inhibit... -
Unchecked EC50 = 10300.0 nM 4.99 PUBCHEM_BIOASSAY: Dose response confirmation of small molecule activators of the... -
Unchecked IC50 = 10220.0 nM 4.99 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -
ATP-dependent molecular chaperone HSP82 EC50 = 11235.0 nM 4.95 PUBCHEM_BIOASSAY: Luminescence Cell-Based Secondary Assay to Identify Inhibitors... -
Unchecked EC50 = 16138.0 nM 4.79 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay for toxicity in mammal... -
Unchecked EC50 = 16644.0 nM 4.78 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
BJ EC50 = 21110.0 nM 4.68 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
BJ EC50 = 33713.0 nM 4.47 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Comp... -
Catechol O-methyltransferase IC50 = 58884.37 nM 4.23 Inhibition of Sprague-Dawley rat liver COMT after 10 mins using 0.05 uCi [14CH3]... 817025

Literature References

PubMed DOI Target Context # Activities
401891 10.1021/jm00211a019 No relevant target 5
812992 10.1021/jm00223a031 Streptococcus mutans 4
817025 10.1021/jm00226a025 Catechol O-methyltransferase 1
812992 10.1021/jm00223a031 No relevant target 1
- 10.6019/CHEMBL4296182 Staphylococcus aureus 1
- 10.6019/CHEMBL4296182 Escherichia coli 1
- 10.6019/CHEMBL4296182 Klebsiella pneumoniae 1
- 10.6019/CHEMBL4296182 Pseudomonas aeruginosa 1
- 10.6019/CHEMBL4296182 Candida albicans 1
- 10.6019/CHEMBL4296182 HEK293 1
- 10.6019/CHEMBL4296182 Acinetobacter baumannii 1
- 10.6019/CHEMBL4296182 Cryptococcus neoformans 1
33901770 10.1016/j.bmc.2021.116160 Indoleamine 2,3-dioxygenase 1 1
33901770 10.1016/j.bmc.2021.116160 Tryptophan 2,3-dioxygenase 1
33901770 10.1016/j.bmc.2021.116160 Unchecked 1

Data from ChEMBL 36 via Core Engine