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Compound Detail

CHEMBL3640337

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COc1ccc2c(c1)C(=O)N(C[C@@]1(C#Cc3ccc(-c4nc(-c5cccnc5)ccc4O)cc3)NC(=O)NC1=O)C2

Basic Information

ChEMBL ID CHEMBL3640337
Phase Preclinical
Structure Type MOL
InChI Key DPNXFCNWZPIWBE-WJOKGBTCSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

545.6
MW (Da)
3.11
ALogP
7
HBA
3
HBD
133.8
PSA (Ų)
0.26
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 C31H23N5O5
MW 545.56
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -0.44

Activity Summary

IC50 1 meas. best 7.1
Ki 1 meas. best 10.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tumor necrosis factor
CHEMBL1825
Ki 10.19 10.19 0.1 1
Tumor necrosis factor
CHEMBL1825
IC50 7.1 7.1 80.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tumor necrosis factor Ki = 0.0651 nM 10.19 Inhibition Assay: Inhibition assay using TNF-alpha. -
Tumor necrosis factor IC50 = 80.25 nM 7.1 Inhibition Assay: Inhibition assay using TNF-alpha. -

Data from ChEMBL 36 via Core Engine