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Compound Detail

CHEMBL3199050

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CC1=C/C(=N\OS(=O)(=O)c2ccccc2)C=CC1=O

Basic Information

ChEMBL ID CHEMBL3199050
Phase Preclinical
Structure Type MOL
InChI Key XTGPABZHVNQSCA-KAMYIIQDSA-N
9
Targets
14
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

277.3
MW (Da)
1.83
ALogP
5
HBA
0
HBD
72.8
PSA (Ų)
0.62
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H11NO4S
MW 277.30
Aromatic Rings 1
Heavy Atoms 19
NP-Likeness -0.01

Activity Summary

IC50 9 meas. best 6.58
EC50 5 meas. best 6.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitochondrial import inner membrane translocase subunit TIM10
CHEMBL1741194
IC50 6.58 6.46 260.0 2
Mitochondrial import inner membrane translocase subunit TIM23
CHEMBL1741180
IC50 6.57 6.57 270.0 1
BJ
CHEMBL614358
EC50 6.27 5.6725 542.0 4
DNA damage-inducible transcript 3 protein
CHEMBL2146304
IC50 5.84 5.84 1430.0 1
Mannose-6-phosphate isomerase
CHEMBL2758
IC50 5.57 5.57 2707.5 1
X-box-binding protein 1
CHEMBL1741176
IC50 5.54 5.54 2900.0 1
Sphingosine 1-phosphate receptor 2
CHEMBL2955
IC50 5.53 5.375 2921.0 2
Unchecked
CHEMBL612545
EC50 5.21 5.21 6187.0 1
DNA dC->dU-editing enzyme APOBEC-3G
CHEMBL1741217
IC50 5.13 5.13 7430.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitochondrial import inner membrane translocase subunit TIM10 IC50 = 260.0 nM 6.58 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS small molecule inhibitors o... -
Mitochondrial import inner membrane translocase subunit TIM23 IC50 = 270.0 nM 6.57 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS small molecule inhibitors o... -
Mitochondrial import inner membrane translocase subunit TIM10 IC50 = 460.0 nM 6.34 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS small molecule inhibitors o... -
BJ EC50 = 542.0 nM 6.27 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Dose Response to Characterize Compound... -
DNA damage-inducible transcript 3 protein IC50 = 1430.0 nM 5.84 PUBCHEM_BIOASSAY: CHOP dose-response primary assay. (Class of assay: confirmator... -
BJ EC50 = 2563.0 nM 5.59 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Mannose-6-phosphate isomerase IC50 = 2707.5 nM 5.57 PUBCHEM_BIOASSAY: HTS identification of compounds inhibiting phosphomannose isom... -
X-box-binding protein 1 IC50 = 2900.0 nM 5.54 PUBCHEM_BIOASSAY: XBP1 DR counterscreen for CHOP. (Class of assay: confirmatory)... -
Sphingosine 1-phosphate receptor 2 IC50 = 2921.0 nM 5.53 PUBCHEM_BIOASSAY: Counterscreen for S1P2 Antagonists: Dose Response Cell-Based S... -
BJ EC50 = 3325.0 nM 5.48 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Comp... -
BJ EC50 = 4433.0 nM 5.35 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Sphingosine 1-phosphate receptor 2 IC50 = 5975.0 nM 5.22 PUBCHEM_BIOASSAY: Dose Response Cell Based Assay for Antagonists of the S1P2 Rec... -
Unchecked EC50 = 6187.0 nM 5.21 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
DNA dC->dU-editing enzyme APOBEC-3G IC50 = 7430.0 nM 5.13 PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule APOBEC3G DNA Deam... -

Data from ChEMBL 36 via Core Engine