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Compound Detail

CHEMBL3640299

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COc1ccc2c(c1F)C(=O)N(C[C@@]1(C#Cc3cc(F)c4c(=O)[nH][nH]c4c3)NC(=O)NC1=O)C2

Basic Information

ChEMBL ID CHEMBL3640299
Phase Preclinical
Structure Type MOL
InChI Key LITZWIRLAPNJMW-JOCHJYFZSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

467.4
MW (Da)
0.73
ALogP
5
HBA
4
HBD
136.4
PSA (Ų)
0.33
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 C22H15F2N5O5
MW 467.39
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.38

Activity Summary

IC50 1 meas. best 6.42
Ki 1 meas. best 10.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tumor necrosis factor
CHEMBL1825
Ki 10.52 10.52 0.0 1
Tumor necrosis factor
CHEMBL1825
IC50 6.42 6.42 383.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tumor necrosis factor Ki = 0.03 nM 10.52 Inhibition Assay: Inhibition assay using TNF-alpha. -
Tumor necrosis factor IC50 = 383.45 nM 6.42 Inhibition Assay: Inhibition assay using TNF-alpha. -

Data from ChEMBL 36 via Core Engine