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Compound Detail

CHEMBL4877695

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O=C1NCc2sccc2C2=CN=C(NCc3c(F)ccc4c3CCO4)N3C=NC1C23

Basic Information

ChEMBL ID CHEMBL4877695
Phase Preclinical
Structure Type MOL
InChI Key HMRIVVIJEQLJHN-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

423.5
MW (Da)
2.03
ALogP
7
HBA
2
HBD
78.3
PSA (Ų)
0.78
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H18FN5O2S
MW 423.47
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.27

Activity Summary

IC50 2 meas. best 8.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
KARPAS-422
CHEMBL2366368
IC50 8.18 8.18 6.6 1
Polycomb protein EED
CHEMBL2189117
IC50 7.95 7.95 11.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34613724 10.1021/acs.jmedchem.1c01059 KARPAS-422 1
34613724 10.1021/acs.jmedchem.1c01059 Polycomb protein EED 1

Data from ChEMBL 36 via Core Engine