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Compound Detail

CHEMBL3642548

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COc1ccc2c(c1)C(=O)N(C[C@@]1(C#Cc3cccnc3N3CCOCC3)NC(=O)NC1=O)C2

Basic Information

ChEMBL ID CHEMBL3642548
Phase Preclinical
Structure Type MOL
InChI Key GFIGHPAFLJOFHC-XMMPIXPASA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

461.5
MW (Da)
0.51
ALogP
7
HBA
2
HBD
113.1
PSA (Ų)
0.50
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 C24H23N5O5
MW 461.48
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.79

Activity Summary

IC50 1 meas. best 6.2
Ki 1 meas. best 9.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tumor necrosis factor
CHEMBL1825
Ki 9.72 9.72 0.2 1
Tumor necrosis factor
CHEMBL1825
IC50 6.2 6.2 633.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tumor necrosis factor Ki = 0.19 nM 9.72 Inhibition Assay: Inhibition assay using TNF-alpha. -
Tumor necrosis factor IC50 = 633.0 nM 6.2 Inhibition Assay: Inhibition assay using TNF-alpha. -

Data from ChEMBL 36 via Core Engine