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Compound Detail

CHEMBL3108947

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CC(/C=C/[C@@H]1C[C@]2(CO2)CC(C)(C)O1)=C\C[C@H]1CC[C@@H](NC(=O)/C=C\[C@H](C)OC(=O)N(C)C)CC1

Basic Information

ChEMBL ID CHEMBL3108947
Phase Preclinical
Structure Type MOL
InChI Key HPIIOCDKJSVOBG-ORMXYABYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

488.7
MW (Da)
4.92
ALogP
5
HBA
1
HBD
80.4
PSA (Ų)
0.30
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H44N2O5
MW 488.67
Aromatic Rings 0
Heavy Atoms 35
NP-Likeness 1.06

Activity Summary

IC50 1 meas. best 7.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NON-PROTEIN TARGET
CHEMBL3879801
IC50 7.39 7.39 41.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
NON-PROTEIN TARGET IC50 = 41.0 nM 7.39 Cytotoxicity against human JeKo1 cells after 72 hrs by CellTiter-Glo assay 24325474

Literature References

PubMed DOI Target Context # Activities
24325474 10.1021/jm401370h SK-MEL-2 9
24325474 10.1021/jm401370h NON-PROTEIN TARGET 2
24325474 10.1021/jm401370h HeLa 2
24325474 10.1021/jm401370h No relevant target 1
24325474 10.1021/jm401370h Unchecked 1
24325474 10.1021/jm401370h Plasma 1
24325474 10.1021/jm401370h PC-3 1
24325474 10.1021/jm401370h SK-N-AS 1
24325474 10.1021/jm401370h WiDr 1
28049589 10.1016/j.bmcl.2016.12.056 Dual specificity protein kinase CLK1 1

Data from ChEMBL 36 via Core Engine