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Compound Detail

CHEMBL5286474

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Cc1nc2cc(-c3cc(C(=O)NCCO)ccc3Oc3ccc(F)cc3F)ccc2[nH]c1=O

Basic Information

ChEMBL ID CHEMBL5286474
Phase Preclinical
Structure Type MOL
InChI Key VBSXZLUOPFVFLH-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

451.4
MW (Da)
3.69
ALogP
5
HBA
3
HBD
104.3
PSA (Ų)
0.41
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H19F2N3O4
MW 451.43
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.25

Activity Summary

IC50 3 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HT-29
CHEMBL384
IC50 7.82 7.82 15.1 1
HepG2
CHEMBL395
IC50 7.75 7.75 17.9 1
Bromodomain-containing protein 4
CHEMBL1163125
IC50 6.21 6.21 620.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
36599264 10.1016/j.bmc.2022.117152 Bromodomain-containing protein 4 2
36599264 10.1016/j.bmc.2022.117152 MCF7 1
36599264 10.1016/j.bmc.2022.117152 HepG2 1
36599264 10.1016/j.bmc.2022.117152 HT-29 1
36599264 10.1016/j.bmc.2022.117152 GES1 1

Data from ChEMBL 36 via Core Engine