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Compound Detail

CHEMBL1701224

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O=C(O)COc1ccc(/C=N/NC(=O)c2ccc(-c3csc(Nc4ccc(Cl)cc4)n3)cc2)cc1

Basic Information

ChEMBL ID CHEMBL1701224
Phase Preclinical
Structure Type MOL
InChI Key TXWSATBBJRPVTL-UVHMKAGCSA-N
9
Targets
18
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

507.0
MW (Da)
5.43
ALogP
7
HBA
3
HBD
112.9
PSA (Ų)
0.21
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H19ClN4O4S
MW 506.97
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.94

Activity Summary

IC50 18 meas. best 6.95

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein phosphatase non-receptor type 22
CHEMBL2889
IC50 6.95 6.1775 113.0 8
Tyrosine-protein phosphatase non-receptor type 7
CHEMBL2219
IC50 6.71 6.71 193.0 1
Tyrosine-protein phosphatase non-receptor type 12
CHEMBL3236
IC50 6.49 6.485 325.0 2
Induced myeloid leukemia cell differentiation protein Mcl-1
CHEMBL4361
IC50 6.05 6.05 886.4 1
Dual specificity protein phosphatase 3
CHEMBL2635
IC50 5.89 5.745 1300.0 2
Voltage-gated N-type calcium channel alpha-1B subunit/Amyloid beta A4 precursor protein-binding family A member 1
CHEMBL2097170
IC50 5.0 5.0 10100.0 1
Envelope glycoprotein gp160
CHEMBL1293311
IC50 4.82 4.82 15000.0 1
Dual specificity protein phosphatase 6
CHEMBL5511
IC50 4.56 4.56 27300.0 1
Hexokinase HKDC1
CHEMBL1741200
IC50 4.48 4.48 33000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 113.0 nM 6.95 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using pCAP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 7 IC50 = 193.0 nM 6.71 PUBCHEM_BIOASSAY: SAR analysis of compounds that inhibit HePTP - Set 2. (Class o... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 249.0 nM 6.6 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using pCAP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 12 IC50 = 325.0 nM 6.49 PUBCHEM_BIOASSAY: SAR Selectivity Analysis of small molecule inhibitors of PEST ... -
Tyrosine-protein phosphatase non-receptor type 12 IC50 = 334.0 nM 6.48 PUBCHEM_BIOASSAY: SAR Selectivity Analysis of small molecule inhibitors of PEST ... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 369.0 nM 6.43 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using pCAP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 527.0 nM 6.28 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using pCAP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 626.0 nM 6.2 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using OMFP substrate for In Vitro d... -
Induced myeloid leukemia cell differentiation protein Mcl-1 IC50 = 886.38 nM 6.05 PUBCHEM_BIOASSAY: Dose Response Confirmation for Mcl-1/Noxa Interaction Inhibito... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 1240.0 nM 5.91 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using OMFP substrate for In Vitro d... -
Dual specificity protein phosphatase 3 IC50 = 1300.0 nM 5.89 PUBCHEM_BIOASSAY: Fluorescent assay for identification of compounds that inhibit... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 1470.0 nM 5.83 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using OMFP substrate for In Vitro d... -
Dual specificity protein phosphatase 3 IC50 = 2520.0 nM 5.6 PUBCHEM_BIOASSAY: uHTS absorbance assay for the identification of compounds that... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 6069.0 nM 5.22 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using OMFP substrate for In Vitro d... -
Voltage-gated N-type calcium channel alpha-1B subunit/Amyloid beta A4 precursor protein-binding family A member 1 IC50 = 10100.0 nM 5.0 PUBCHEM_BIOASSAY: Homogeneous Time-Resolved Fluorescence Resonance Energy Transf... -
Envelope glycoprotein gp160 IC50 = 15000.0 nM 4.82 PUBCHEM_BIOASSAY: uHTS fluorescence assay for the identification of Human Immuno... -
Dual specificity protein phosphatase 6 IC50 = 27300.0 nM 4.56 PUBCHEM_BIOASSAY: MKP-3 in vitro HTS assay. (Class of assay: confirmatory) [Rela... -
Hexokinase HKDC1 IC50 = 33000.0 nM 4.48 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of hexokinase domain ... -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1

Data from ChEMBL 36 via Core Engine