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Compound Detail

CHEMBL1382917

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CCN1/C(=C\c2ccc3ccccc3[n+]2CC)Sc2cc(C)ccc21.[I-]

Basic Information

ChEMBL ID CHEMBL1382917
Phase Preclinical
Structure Type MOL
InChI Key UOHMZCIULLCGBK-UHFFFAOYSA-M
Parent Compound CHEMBL1618929
Active Moiety CHEMBL1618929
10
Targets
16
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

347.5
MW (Da)
5.39
ALogP
2
HBA
0
HBD
7.1
PSA (Ų)
0.59
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23IN2S
MW 474.41
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.04

Activity Summary

IC50 15 meas. best 6.2
EC50 1 meas. best 4.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.2 4.9867 630.0 3
COUP transcription factor 2
CHEMBL1961790
IC50 5.56 5.56 2750.0 1
Candida albicans
CHEMBL366
IC50 5.55 5.55 2800.0 3
Jurkat
CHEMBL397
IC50 4.81 4.81 15500.0 1
Unchecked
CHEMBL612545
EC50 4.8 4.8 15670.0 1
Intestinal-type alkaline phosphatase
CHEMBL5573
IC50 4.79 4.71 16100.0 2
Intestinal-type alkaline phosphatase
CHEMBL3151
IC50 4.68 4.68 20800.0 1
Alkaline phosphatase, germ cell type
CHEMBL3402
IC50 4.55 4.55 28200.0 1
Alkaline phosphatase, tissue-nonspecific isozyme
CHEMBL5979
IC50 4.54 4.54 28600.0 1
Tegument protein VP16
CHEMBL4218
IC50 4.27 4.27 53929.0 1
Exodeoxyribonuclease V
CHEMBL2095232
IC50 4.14 4.14 72809.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 630.0 nM 6.2 PUBCHEM_BIOASSAY: Dose response counterscreen of uHTS chemical inhibitors of bot... -
COUP transcription factor 2 IC50 = 2750.0 nM 5.56 PubChem BioAssay. Luminescence-based cell-based high throughput dose response as... -
Candida albicans IC50 = 2800.0 nM 5.55 Antibiofilm activity against fluconazole-resistant Candida albicans 29E clinical... 28051303
Candida albicans IC50 = 2800.0 nM 5.55 Antibiofilm activity against Candida albicans SC5314 after 48 hrs by Alamar blue... 28051303
Candida albicans IC50 = 2800.0 nM 5.55 Antibiofilm activity against Candida albicans CAF2-1 after 48 hrs by Alamar blue... 28051303
Jurkat IC50 = 15500.0 nM 4.81 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS of chemical inhibitors of b... -
Unchecked EC50 = 15670.0 nM 4.8 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Acti... -
Intestinal-type alkaline phosphatase IC50 = 16100.0 nM 4.79 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS hits from a small molecule ... -
Intestinal-type alkaline phosphatase IC50 = 20800.0 nM 4.68 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS inhibitors of Human Intesti... -
Intestinal-type alkaline phosphatase IC50 = 23500.0 nM 4.63 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS hits from a small molecule ... -
Alkaline phosphatase, germ cell type IC50 = 28200.0 nM 4.55 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS inhibitors of Human Intesti... -
Alkaline phosphatase, tissue-nonspecific isozyme IC50 = 28600.0 nM 4.54 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS inhibitors of Human Intesti... -
Unchecked IC50 = 37456.0 nM 4.43 PUBCHEM_BIOASSAY: Counterscreen for AddAB inhibitors: absorbance-based bacterial... -
Unchecked IC50 = 47297.0 nM 4.33 PUBCHEM_BIOASSAY: Absorbance-based bacterial cell-based high throughput dose res... -
Tegument protein VP16 IC50 = 53929.0 nM 4.27 PubChem BioAssay. Counterscreen for inhibitors of COUP-TFII (NR2F2): Luminescenc... -
Exodeoxyribonuclease V IC50 = 72809.0 nM 4.14 PUBCHEM_BIOASSAY: Counterscreen for AddAB inhibitors: absorbance-based bacterial... -

Literature References

PubMed DOI Target Context # Activities
28051303 10.1021/acs.jmedchem.6b01203 Candida albicans 3

Data from ChEMBL 36 via Core Engine