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Compound Detail

CHEMBL1569585

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C=C1C(=O)C=C2CN(C(=O)c3ccccc3)[C@@](Cc3ccc(F)cc3)(C(=O)OC)[C@@H]12

Basic Information

ChEMBL ID CHEMBL1569585
Phase Preclinical
Structure Type MOL
InChI Key OAFVCCUNRXBEEH-XUZZJYLKSA-N
7
Targets
13
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

405.4
MW (Da)
3.12
ALogP
4
HBA
0
HBD
63.7
PSA (Ų)
0.58
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 C24H20FNO4
MW 405.43
Aromatic Rings 2
Heavy Atoms 30

Activity Summary

IC50 8 meas. best 6.33
EC50 5 meas. best 6.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
BJ
CHEMBL614358
EC50 6.48 5.9433 333.0 3
Sphingosine 1-phosphate receptor 4
CHEMBL3230
IC50 6.33 5.88 473.0 2
Unchecked
CHEMBL612545
EC50 6.18 6.18 662.0 1
Unchecked
CHEMBL612545
IC50 6.05 5.67 890.0 3
X-box-binding protein 1
CHEMBL1741176
IC50 5.99 5.99 1030.0 1
Mucolipin-3
CHEMBL1293243
EC50 5.95 5.95 1120.0 1
DNA damage-inducible transcript 3 protein
CHEMBL2146304
IC50 5.94 5.94 1160.0 1
Sphingosine 1-phosphate receptor 1
CHEMBL4333
IC50 4.92 4.92 11970.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
BJ EC50 = 333.0 nM 6.48 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Sphingosine 1-phosphate receptor 4 IC50 = 473.0 nM 6.33 PUBCHEM_BIOASSAY: Fluorescence dose response cell-based high throughput screenin... -
BJ EC50 = 554.0 nM 6.26 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked EC50 = 662.0 nM 6.18 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked IC50 = 890.0 nM 6.05 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS chemical inhibitors of T-ce... -
Unchecked IC50 = 1010.0 nM 6.0 PUBCHEM_BIOASSAY: Dose Response selectivity of uHTS chemical inhibitors of T-cel... -
X-box-binding protein 1 IC50 = 1030.0 nM 5.99 PUBCHEM_BIOASSAY: XBP1 DR counterscreen for CHOP. (Class of assay: confirmatory)... -
Mucolipin-3 EC50 = 1120.0 nM 5.95 PUBCHEM_BIOASSAY: Fluorescence counterscreen assay for TRPN1 agonists: dose resp... -
DNA damage-inducible transcript 3 protein IC50 = 1160.0 nM 5.94 PUBCHEM_BIOASSAY: CHOP dose-response primary assay. (Class of assay: confirmator... -
Sphingosine 1-phosphate receptor 4 IC50 = 3697.0 nM 5.43 PUBCHEM_BIOASSAY: Late stage fluorescence dose response cell-based screening ass... -
BJ EC50 = 8079.0 nM 5.09 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Comp... -
Unchecked IC50 = 11000.0 nM 4.96 PUBCHEM_BIOASSAY: Dose response counterscreen of uHTS chemical inhibitors of T-c... -
Sphingosine 1-phosphate receptor 1 IC50 = 11970.0 nM 4.92 PUBCHEM_BIOASSAY: Fluorescence-based counterscreen assay for S1P4 antagonists: C... -

Data from ChEMBL 36 via Core Engine