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Compound Detail

CHEMBL519243

HOLACANTHONE
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CC(=O)O[C@H]1C(=O)O[C@@H]2C[C@H]3C(C)=CC(=O)[C@@H](O)[C@]3(C)[C@H]3[C@]4(O)OC[C@]32[C@@H]1[C@@H](C)[C@H]4O

Basic Information

ChEMBL ID CHEMBL519243
Name HOLACANTHONE
Phase Preclinical
Structure Type MOL
InChI Key OFHVBIQKCNMHKC-ISEFROCLSA-N
1
Targets
3
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

436.5
MW (Da)
-0.29
ALogP
9
HBA
3
HBD
139.6
PSA (Ų)
0.47
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C22H28O9
MW 436.46
Aromatic Rings 0
Heavy Atoms 31
NP-Likeness 4.08

Activity Summary

IC50 2 meas. best 6.7
EC50 1 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HL-60
CHEMBL383
EC50 6.7 6.7 200.0 1
HL-60
CHEMBL383
IC50 6.7 6.5 200.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0926-6690(99)00003-5 Reticulitermes flavipes 5
6619884 10.1021/np50027a011 P388 5
11754601 10.1021/np010212p HL-60 4
8984156 10.1021/np960013j Plasmodium falciparum 2
8984156 10.1021/np960013j SK-OV-3 1
- 10.1007/s00044-011-9767-1 Entamoeba histolytica 1
19199792 10.1021/np800732n Transcription factor Jun 1
19199792 10.1021/np800732n Unchecked 1
19199792 10.1021/np800732n HeLa 1
19199792 10.1021/np800732n NON-PROTEIN TARGET 1
18834112 10.1021/jm800656v Amine oxidase [flavin-containing] B 1
18834112 10.1021/jm800656v Amine oxidase [flavin-containing] A 1
7130986 10.1021/np50022a010 KB 1
8984156 10.1021/np960013j Vero 1
3110376 10.1021/np50049a003 Bacillus subtilis 1
8984156 10.1021/np960013j BT-549 1
8984156 10.1021/np960013j KB 1
8984156 10.1021/np960013j K562 1
6619884 10.1021/np50027a011 KB 1
7264678 10.1021/np50015a007 P388 1

Data from ChEMBL 36 via Core Engine