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Compound Detail

CHEMBL5715246

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CC(C)N(CCCNC(=O)Nc1ccc(C(C)(C)C)cc1)C[C@H]1O[C@@H](n2cc(Br)c3c(N)ncnc32)[C@H](O)[C@@H]1O.Cl

Basic Information

ChEMBL ID CHEMBL5715246
Phase Preclinical
Structure Type MOL
InChI Key CREBMQZPDVWTPT-DGUBOJIQSA-N
Parent Compound CHEMBL3087498
Active Moiety CHEMBL3087498
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

618.6
MW (Da)
3.61
ALogP
9
HBA
5
HBD
150.8
PSA (Ų)
0.23
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug Chemical Probe

Extended Properties

Molecular Formula C28H41BrClN7O4
MW 655.04
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -0.70

Activity Summary

IC50 1 meas. best 5.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
FLC clone 745
CHEMBL6066809
IC50 5.64 5.64 2300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
FLC clone 745 IC50 = 2300.0 nM 5.64 Cytotoxicity against mouse FLC clone 745 cells assessed as reduction in cell via... 33407944

Literature References

PubMed DOI Target Context # Activities
33407944 10.1186/s40709-020-00132-3 FLC clone 745 2
33407944 10.1186/s40709-020-00132-3 Histone-lysine N-methyltransferase, H3 lysine-79 specific 2

Data from ChEMBL 36 via Core Engine