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Compound Detail

CHEMBL3642485

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COc1ccc2c(c1)C(=O)N(C[C@@]1(C#Cc3ccc(C4(C5CCC5)NC(=O)NC4=O)cc3)NC(=O)NC1=O)C2

Basic Information

ChEMBL ID CHEMBL3642485
Phase Preclinical
Structure Type MOL
InChI Key VLYULZSNSXSWHO-QXPUDEPPSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

527.5
MW (Da)
1.12
ALogP
6
HBA
4
HBD
145.9
PSA (Ų)
0.34
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H25N5O6
MW 527.54
Aromatic Rings 2
Heavy Atoms 39
NP-Likeness -0.08

Activity Summary

IC50 1 meas. best 6.42
Ki 1 meas. best 9.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tumor necrosis factor
CHEMBL1825
Ki 9.77 9.77 0.2 1
Tumor necrosis factor
CHEMBL1825
IC50 6.42 6.42 382.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tumor necrosis factor Ki = 0.17 nM 9.77 Inhibition Assay: Inhibition assay using TNF-alpha. -
Tumor necrosis factor IC50 = 382.0 nM 6.42 Inhibition Assay: Inhibition assay using TNF-alpha. -

Data from ChEMBL 36 via Core Engine