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Compound Detail

CHEMBL1371816

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N#C/C(=C\c1ccc(OCc2ccc(Cl)cc2)cc1)C(=O)Nc1cccc(C(=O)O)c1

Basic Information

ChEMBL ID CHEMBL1371816
Phase Preclinical
Structure Type MOL
InChI Key QXRVNDCFCHMEAR-XDHOZWIPSA-N
6
Targets
17
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

432.9
MW (Da)
5.16
ALogP
4
HBA
2
HBD
99.4
PSA (Ų)
0.40
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H17ClN2O4
MW 432.86
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.16

Activity Summary

IC50 14 meas. best 6.19
EC50 3 meas. best 4.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein phosphatase non-receptor type 7
CHEMBL2219
IC50 6.19 5.3767 651.0 3
Tyrosine-protein phosphatase non-receptor type 12
CHEMBL3236
IC50 5.54 5.54 2910.0 1
Tyrosine-protein phosphatase non-receptor type 22
CHEMBL2889
IC50 5.42 5.139 3770.0 10
Heat shock factor protein 1
CHEMBL5313
EC50 4.96 4.96 10920.0 1
Unchecked
CHEMBL612545
EC50 4.81 4.81 15600.0 1
Apoptotic protease-activating factor 1
CHEMBL1795093
EC50 4.68 4.68 20800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein phosphatase non-receptor type 7 IC50 = 651.0 nM 6.19 PUBCHEM_BIOASSAY: SAR analysis of compounds that inhibit HePTP - Set 2. (Class o... -
Tyrosine-protein phosphatase non-receptor type 12 IC50 = 2910.0 nM 5.54 PUBCHEM_BIOASSAY: SAR Selectivity Analysis of small molecule inhibitors of PEST ... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 3770.0 nM 5.42 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using OMFP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 4740.0 nM 5.32 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using OMFP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 4957.0 nM 5.3 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using pCAP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 6360.0 nM 5.2 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using pCAP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 6424.0 nM 5.19 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS hits from a small molecule ... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 6540.0 nM 5.18 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using pCAP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 6862.0 nM 5.16 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS hits from a small molecule ... -
Tyrosine-protein phosphatase non-receptor type 7 IC50 = 7880.0 nM 5.1 PUBCHEM_BIOASSAY: HTS HePTP Fluorescent Assay using OMFP substrate for In Vitro ... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 8283.5 nM 5.08 PUBCHEM_BIOASSAY: LYP1 Fluorescent Assay using OMFP substrate for In Vitro dose ... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 8615.61 nM 5.07 PUBCHEM_BIOASSAY: uHTS identification of small molecule inhibitors of LYP via a ... -
Heat shock factor protein 1 EC50 = 10920.0 nM 4.96 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Retest to Identify Potentiators o... -
Tyrosine-protein phosphatase non-receptor type 7 IC50 = 14604.0 nM 4.84 PUBCHEM_BIOASSAY: Dose Response confirmation of HTS hits from an HePTP Fluoresce... -
Unchecked EC50 = 15600.0 nM 4.81 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 activators ... -
Apoptotic protease-activating factor 1 EC50 = 20800.0 nM 4.68 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS Activators of the Apaf-1 Pa... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 34166.0 nM 4.47 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using OMFP substrate for In Vitro d... -

Data from ChEMBL 36 via Core Engine