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Compound Detail

CHEMBL1215677

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CC(C)c1cc(C(=O)N2Cc3ccc(OCCN(C)C)cc3C2)c(O)cc1O

Basic Information

ChEMBL ID CHEMBL1215677
Phase Preclinical
Structure Type MOL
InChI Key QVVRLPMMRCAKBP-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

384.5
MW (Da)
3.32
ALogP
5
HBA
2
HBD
73.2
PSA (Ų)
0.80
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H28N2O4
MW 384.48
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.57

Activity Summary

IC50 1 meas. best 7.68
Kd 1 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Kd 9.3 9.3 0.5 1
HCT-116
CHEMBL394
IC50 7.68 7.68 21.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 170.0 mL.min-1.kg-1 Mus musculus
CL 0.034 mL.min-1.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20662534 10.1021/jm100060b HCT-116 4
20662534 10.1021/jm100060b Voltage-gated inwardly rectifying potassium channel KCNH2 2
20662534 10.1021/jm100060b No relevant target 2
20662534 10.1021/jm100060b ADMET 2
20662534 10.1021/jm100060b Mus musculus 1
20662534 10.1021/jm100060b Unchecked 1
20662534 10.1021/jm100060b Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine