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Compound Detail

CHEMBL5423622

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Cc1cc(C)c(CNC(=O)c2cc(-c3ccc(N4CCN(C(=O)C[C@@H]5N=C(c6ccc(Cl)cc6)c6c(sc(C)c6C)-n6c(C)nnc65)CC4)cc3)cc3c2cnn3C(C)C)c(=O)[nH]1

Basic Information

ChEMBL ID CHEMBL5423622
Phase Preclinical
Structure Type MOL
InChI Key IETSGFYKFVUIOC-FAIXQHPJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

881.5
MW (Da)
8.37
ALogP
11
HBA
2
HBD
146.4
PSA (Ų)
0.15
QED
3
Ro5 Violations
9
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C48H49ClN10O3S
MW 881.51
Aromatic Rings 7
Heavy Atoms 63
NP-Likeness -1.43

Activity Summary

IC50 1 meas. best 4.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HCT-116
CHEMBL394
IC50 4.75 4.75 17760.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
HCT-116 IC50 = 17760.0 nM 4.75 Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by M... 37379621

Literature References

PubMed DOI Target Context # Activities
37379621 10.1016/j.bmc.2023.117386 Bromodomain-containing protein 4 2
37379621 10.1016/j.bmc.2023.117386 HCT-116 1
37379621 10.1016/j.bmc.2023.117386 MDA-MB-231 1
37379621 10.1016/j.bmc.2023.117386 BT-549 1
37379621 10.1016/j.bmc.2023.117386 A549 1

Data from ChEMBL 36 via Core Engine