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Compound Detail

CHEMBL1427185

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O=C1C=CC(=O)N1CCNc1ncc(C(F)(F)F)cc1Cl

Basic Information

ChEMBL ID CHEMBL1427185
Phase Preclinical
Structure Type MOL
InChI Key XRJVXAMPYWOKBH-UHFFFAOYSA-N
11
Targets
17
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

319.7
MW (Da)
2.09
ALogP
4
HBA
1
HBD
62.3
PSA (Ų)
0.86
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 C12H9ClF3N3O2
MW 319.67
Aromatic Rings 1
Heavy Atoms 21
NP-Likeness -1.61

Activity Summary

IC50 13 meas. best 6.42
EC50 4 meas. best 5.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.42 5.62 383.0 2
Voltage-gated N-type calcium channel alpha-1B subunit/Amyloid beta A4 precursor protein-binding family A member 1
CHEMBL2097170
IC50 5.82 5.37 1530.0 2
CHO
CHEMBL613853
IC50 5.79 5.79 1625.0 1
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 5.75 5.75 1760.0 1
Unchecked
CHEMBL612545
EC50 5.55 5.475 2783.0 2
Toll-like receptor 9
CHEMBL5804
IC50 5.15 5.15 7134.0 1
Beta Lactamase
CHEMBL1293246
IC50 5.1 5.1 7938.0 1
Streptokinase A
CHEMBL1293228
EC50 4.98 4.98 10409.0 1
Streptococcus sp. 'group A'
CHEMBL612389
EC50 4.98 4.98 10380.0 1
Melanocortin receptor 4
CHEMBL259
IC50 4.91 4.91 12255.0 1
C-C chemokine receptor type 6
CHEMBL4423
IC50 4.8 4.8 15900.0 1
Glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase
CHEMBL1741212
IC50 4.7 4.4467 20000.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 383.0 nM 6.42 PUBCHEM_BIOASSAY: Luminescent dose response cell-based high throughput screening... -
Voltage-gated N-type calcium channel alpha-1B subunit/Amyloid beta A4 precursor protein-binding family A member 1 IC50 = 1530.0 nM 5.82 PUBCHEM_BIOASSAY: uHTS Homogeneous Terbium Time-Resolved Fluorescence Resonance ... -
CHO IC50 = 1625.0 nM 5.79 PUBCHEM_BIOASSAY: Counterscreen for inhibitors of TLR9-MyD88 binding: Luminescen... -
Tyrosine-protein kinase JAK2 IC50 = 1760.0 nM 5.75 PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2... -
Unchecked EC50 = 2783.0 nM 5.55 PUBCHEM_BIOASSAY: Luminescence Cell-Based/Microorganism Dose Confirmation HTS to... -
Unchecked EC50 = 3975.0 nM 5.4 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS Screen to Identify C... -
Toll-like receptor 9 IC50 = 7134.0 nM 5.15 PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response as... -
Beta Lactamase IC50 = 7938.0 nM 5.1 PUBCHEM_BIOASSAY: Counterscreen for inhibitors of TLR9-MyD88 binding: fluorescen... -
Streptokinase A EC50 = 10409.0 nM 4.98 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptococcus sp. 'group A' EC50 = 10380.0 nM 4.98 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Voltage-gated N-type calcium channel alpha-1B subunit/Amyloid beta A4 precursor protein-binding family A member 1 IC50 = 12000.0 nM 4.92 PUBCHEM_BIOASSAY: Homogeneous Time-Resolved Fluorescence Resonance Energy Transf... -
Melanocortin receptor 4 IC50 = 12255.0 nM 4.91 PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay fo... -
Unchecked IC50 = 15122.0 nM 4.82 PUBCHEM_BIOASSAY: Counterscreen for biased ligands (antagonists) of the melanoco... -
C-C chemokine receptor type 6 IC50 = 15900.0 nM 4.8 PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of th... -
Glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase IC50 = 20000.0 nM 4.7 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS small molecule inhibitors o... -
Glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase IC50 = 34800.0 nM 4.46 PUBCHEM_BIOASSAY: Dose Response orthogonal kinetic assay utilizing the direct de... -
Glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase IC50 = 65400.0 nM 4.18 PUBCHEM_BIOASSAY: Dose Response orthogonal assay utilizing the direct end-point ... -

Data from ChEMBL 36 via Core Engine