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Compound Detail

CHEMBL421734

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CCC1=C(C)c2nc1cc1[nH]c(c(C)c1CC)c(-c1cc[n+](C)cc1)c1[nH]c(cc3nc(c2-c2cc[n+](C)cc2)C(C)=C3CC)c(CC)c1C.[I-].[I-]

Basic Information

ChEMBL ID CHEMBL421734
Phase Preclinical
Structure Type MOL
InChI Key CNIKDLALWVUVMB-MFEFFYHXSA-M
Parent Compound CHEMBL1185569
Active Moiety CHEMBL1185569
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

662.9
MW (Da)
9.72
ALogP
2
HBA
2
HBD
65.1
PSA (Ų)
0.18
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C44H50I2N6
MW 916.73
Aromatic Rings 5
Heavy Atoms 50
NP-Likeness 0.12

Activity Summary

IC50 1 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
THP-1
CHEMBL614245
IC50 7.92 7.92 12.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
THP-1 IC50 = 12.0 nM 7.92 Concentration for 50% reduction in THp-1 cell numbers, expressed as IC50 15109655

Literature References

PubMed DOI Target Context # Activities
15109655 10.1016/j.bmcl.2004.02.083 THP-1 1

Data from ChEMBL 36 via Core Engine