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Compound Detail

CHEMBL1807705

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CN1CCc2ccc(Nc3nccc(-c4c(-c5cccc(C(=O)Nc6c(F)cccc6F)c5)nc5ccccn45)n3)cc2C1.Cl

Basic Information

ChEMBL ID CHEMBL1807705
Phase Preclinical
Structure Type MOL
InChI Key YKLAEILKLZLJBE-UHFFFAOYSA-N
Parent Compound CHEMBL1851817
Active Moiety CHEMBL1851817
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

587.6
MW (Da)
6.72
ALogP
7
HBA
2
HBD
87.5
PSA (Ų)
0.23
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H28ClF2N7O
MW 624.09
Aromatic Rings 6
Heavy Atoms 44
NP-Likeness -1.68

Activity Summary

IC50 1 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase B-raf
CHEMBL5145
IC50 7.92 7.92 12.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein kinase B-raf IC50 = 12.0 nM 7.92 Inhibition of B-Raf V600E mutant 21733693

Literature References

PubMed DOI Target Context # Activities
21733693 10.1016/j.bmcl.2011.06.021 Serine/threonine-protein kinase B-raf 2
21733693 10.1016/j.bmcl.2011.06.021 SK-MEL-28 1

Data from ChEMBL 36 via Core Engine