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Compound Detail

CHEMBL4216380

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CC1(C)CCC(c2ccc(Cl)cc2)=C(CN2CCc3nc(C(=O)NS(=O)(=O)c4ccc(N[C@H](CCN5CCOCC5)CSc5ccccc5)c(S(=O)(=O)C(F)(F)F)c4)sc3C2)C1

Basic Information

ChEMBL ID CHEMBL4216380
Phase Preclinical
Structure Type MOL
InChI Key LVBGCCULSLDQKD-JGCGQSQUSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

952.6
MW (Da)
8.53
ALogP
12
HBA
2
HBD
138.0
PSA (Ų)
0.11
QED
3
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H49ClF3N5O6S4
MW 952.61
Aromatic Rings 4
Heavy Atoms 62
NP-Likeness -1.08

Activity Summary

IC50 2 meas. best 7.88

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bcl-2-like protein 1
CHEMBL4625
IC50 7.88 7.88 13.2 1
Apoptosis regulator Bcl-2
CHEMBL4860
IC50 7.42 7.42 38.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29229225 10.1016/j.bmc.2017.12.001 Apoptosis regulator Bcl-2 1
29229225 10.1016/j.bmc.2017.12.001 Bcl-2-like protein 1 1
29229225 10.1016/j.bmc.2017.12.001 Unchecked 1

Data from ChEMBL 36 via Core Engine