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Compound Detail

CHEMBL1257003

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COc1cc(/C=C(\C#N)C(=O)c2ccc(O)c(O)c2)cc(I)c1O

Basic Information

ChEMBL ID CHEMBL1257003
Phase Preclinical
Structure Type MOL
InChI Key HSRMHXWCTRFVHK-NYYWCZLTSA-N
9
Targets
14
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

437.2
MW (Da)
3.21
ALogP
6
HBA
3
HBD
110.8
PSA (Ų)
0.22
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C17H12INO5
MW 437.19
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -0.02

Activity Summary

IC50 13 meas. best 6.55
EC50 1 meas. best 5.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lethal(3)malignant brain tumor-like protein 1
CHEMBL1287622
IC50 6.55 6.55 282.0 1
Unchecked
CHEMBL612545
IC50 6.12 5.3567 751.7 3
Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha
CHEMBL1795194
IC50 6.0 5.85 1000.0 2
dengue virus type 2
CHEMBL613966
EC50 5.52 5.52 3000.0 1
Intestinal-type alkaline phosphatase
CHEMBL5573
IC50 5.34 5.24 4560.0 2
Intestinal-type alkaline phosphatase
CHEMBL3151
IC50 5.24 5.24 5700.0 1
Alkaline phosphatase, tissue-nonspecific isozyme
CHEMBL5979
IC50 5.23 5.23 5880.0 1
Alkaline phosphatase, germ cell type
CHEMBL3402
IC50 4.81 4.81 15500.0 1
Plasmodium falciparum
CHEMBL364
IC50 4.8 4.8 15848.9 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Lethal(3)malignant brain tumor-like protein 1 IC50 = 282.0 nM 6.55 Inhibition of L3MBTL1 (unknown origin) by AlphaScreen assay 28478342
Unchecked IC50 = 751.72 nM 6.12 PubChem BioAssay. TR-FRET-based biochemical high throughput dose response assay ... -
Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha IC50 = 1000.0 nM 6.0 Inhibition of PI5P4Kalpha (unknown origin) incubated for 15 mins in presence of ... 32184968
Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha IC50 = 2000.0 nM 5.7 Inhibition of PI5P4Kalpha (unknown origin) incubated for 1 hr in presence of ATP... 37252102
dengue virus type 2 EC50 = 3000.0 nM 5.52 Antiviral activity against DENV2 New Guinea C infected in golden hamster BHK-21 ... 36167010
Intestinal-type alkaline phosphatase IC50 = 4560.0 nM 5.34 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS hits from a small molecule ... -
Intestinal-type alkaline phosphatase IC50 = 5700.0 nM 5.24 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS hits from a small molecule ... -
Alkaline phosphatase, tissue-nonspecific isozyme IC50 = 5880.0 nM 5.23 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS inhibitors of Human Intesti... -
Intestinal-type alkaline phosphatase IC50 = 7310.0 nM 5.14 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS hits from a small molecule ... -
Unchecked IC50 = 9086.0 nM 5.04 PubChem BioAssay. Counterscreen for inhibitors of LEDGF/p75-dependent integratio... -
Unchecked IC50 = 12330.0 nM 4.91 PUBCHEM_BIOASSAY: A biochemical assay using the ADP-Hunter methodology, purified... -
Alkaline phosphatase, germ cell type IC50 = 15500.0 nM 4.81 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS inhibitors of Human Intesti... -
Plasmodium falciparum IC50 = 15848.93 nM 4.8 Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 15848.93 nM 4.8 Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR gr... 19734910

Literature References

PubMed DOI Target Context # Activities
19734910 10.1038/nchembio.215 Plasmodium falciparum 2
17417631 10.1038/nchembio873 Unchecked 1
28478342 10.1016/j.ejmech.2017.04.047 Lethal(3)malignant brain tumor-like protein 1 1
32184968 10.1021/acsmedchemlett.9b00402 Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha 1
37252102 10.1039/d3md00039g Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha 1
36167010 10.1016/j.ejmech.2022.114753 dengue virus type 2 1

Data from ChEMBL 36 via Core Engine