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Compound Detail

CHEMBL1504701

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O=C(NC(Nc1nc2ccc([N+](=O)[O-])cc2s1)(C(F)(F)F)C(F)(F)F)c1ccccc1

Basic Information

ChEMBL ID CHEMBL1504701
Phase Preclinical
Structure Type MOL
InChI Key RVALRXZLYFQZGR-UHFFFAOYSA-N
5
Targets
14
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

464.4
MW (Da)
4.87
ALogP
6
HBA
2
HBD
97.2
PSA (Ų)
0.24
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H10F6N4O3S
MW 464.35
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.83

Activity Summary

EC50 10 meas. best 6.41
IC50 4 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sphingosine 1-phosphate receptor 2
CHEMBL2955
IC50 7.0 6.585 101.0 2
Unchecked
CHEMBL612545
EC50 6.41 5.915 394.0 4
Unchecked
CHEMBL612545
IC50 6.14 6.065 720.0 2
BJ
CHEMBL614358
EC50 6.14 5.8525 727.0 4
Neuropeptide Y receptor type 2
CHEMBL4018
EC50 4.5 4.5 31862.0 1
Neuropeptide Y receptor type 1
CHEMBL4777
EC50 4.45 4.45 35337.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sphingosine 1-phosphate receptor 2 IC50 = 101.0 nM 7.0 PUBCHEM_BIOASSAY: Counterscreen for S1P2 Antagonists: Dose Response Cell-Based S... -
Unchecked EC50 = 394.0 nM 6.41 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Unchecked EC50 = 449.0 nM 6.35 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Sphingosine 1-phosphate receptor 2 IC50 = 682.0 nM 6.17 PUBCHEM_BIOASSAY: Dose Response Cell Based Assay for Antagonists of the S1P2 Rec... -
BJ EC50 = 727.0 nM 6.14 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Dose Response to Characterize Compound... -
Unchecked IC50 = 720.0 nM 6.14 PUBCHEM_BIOASSAY: Dose Response selectivity of uHTS chemical inhibitors of T-cel... -
Unchecked IC50 = 1034.0 nM 5.99 PUBCHEM_BIOASSAY: Luminescence-based dose response cell-based high throughput sc... -
BJ EC50 = 1336.0 nM 5.87 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Comp... -
BJ EC50 = 1405.0 nM 5.85 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked EC50 = 1664.0 nM 5.78 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
BJ EC50 = 2845.0 nM 5.55 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked EC50 = 7501.0 nM 5.12 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Neuropeptide Y receptor type 2 EC50 = 31862.0 nM 4.5 PUBCHEM_BIOASSAY: Fluorescence-based cell-based high-throughput dose response as... -
Neuropeptide Y receptor type 1 EC50 = 35337.0 nM 4.45 PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for agonists of NPY-Y2: cell-... -

Data from ChEMBL 36 via Core Engine