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Compound Detail

CHEMBL1318350

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CCN1/C(=C/c2ccc3cc(C)ccc3[n+]2CC)Sc2ccc3sccc3c21.[I-]

Basic Information

ChEMBL ID CHEMBL1318350
Phase Preclinical
Structure Type MOL
InChI Key WXTVEUVKCYUVQQ-UHFFFAOYSA-M
Parent Compound CHEMBL1617424
Active Moiety CHEMBL1617424
10
Targets
19
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

403.6
MW (Da)
6.60
ALogP
3
HBA
0
HBD
7.1
PSA (Ų)
0.36
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 C24H23IN2S2
MW 530.50
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.19

Activity Summary

EC50 16 meas. best 7.34
IC50 3 meas. best 5.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 7.34 5.95 46.0 3
Beta-adrenergic receptor kinase 1
CHEMBL4079
EC50 6.92 6.92 120.0 1
BJ
CHEMBL614358
EC50 6.43 6.07 370.0 4
ATP-dependent molecular chaperone HSP82
CHEMBL1293251
EC50 5.76 5.13 1745.0 2
Streptokinase A
CHEMBL1293228
EC50 5.63 5.63 2339.0 1
Unchecked
CHEMBL612545
IC50 5.51 4.9133 3100.0 3
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.48 5.48 3288.0 1
Streptococcus
CHEMBL612313
EC50 5.35 5.35 4438.0 1
Alkaline phosphatase, tissue-nonspecific isozyme
CHEMBL5979
EC50 4.22 4.22 60600.0 1
Intestinal-type alkaline phosphatase
CHEMBL5573
EC50 4.21 4.21 61800.0 1
Alkaline phosphatase, germ cell type
CHEMBL3402
EC50 4.18 4.18 65300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 46.0 nM 7.34 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Retest of Candida albicans Growth in t... -
Beta-adrenergic receptor kinase 1 EC50 = 120.0 nM 6.92 PUBCHEM_BIOASSAY: Dose Response of inhibitors of GRK2 binding with RNA aptamer, ... -
BJ EC50 = 370.0 nM 6.43 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Dose Response to Characterize Compound... -
BJ EC50 = 966.0 nM 6.01 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Comp... -
BJ EC50 = 1170.0 nM 5.93 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
BJ EC50 = 1228.0 nM 5.91 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked EC50 = 1453.0 nM 5.84 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
ATP-dependent molecular chaperone HSP82 EC50 = 1745.0 nM 5.76 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay to Measure Toxicity of... -
Streptokinase A EC50 = 2339.0 nM 5.63 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Unchecked IC50 = 3100.0 nM 5.51 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS chemical inhibitors of T-ce... -
Streptococcus sp. 'group A' EC50 = 3288.0 nM 5.48 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptococcus EC50 = 4438.0 nM 5.35 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Unchecked IC50 = 9390.0 nM 5.03 PUBCHEM_BIOASSAY: Dose Response selectivity of uHTS chemical inhibitors of T-cel... -
Unchecked EC50 = 21126.0 nM 4.67 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay for toxicity in mammal... -
ATP-dependent molecular chaperone HSP82 EC50 = 31984.0 nM 4.5 PUBCHEM_BIOASSAY: Luminescence Cell-Based Secondary Assay to Identify Inhibitors... -
Alkaline phosphatase, tissue-nonspecific isozyme EC50 = 60600.0 nM 4.22 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS activators of Mouse Intesti... -
Intestinal-type alkaline phosphatase EC50 = 61800.0 nM 4.21 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS activators of Mouse Intesti... -
Unchecked IC50 = 63000.0 nM 4.2 PUBCHEM_BIOASSAY: Dose response counterscreen of uHTS chemical inhibitors of T-c... -
Alkaline phosphatase, germ cell type EC50 = 65300.0 nM 4.18 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS activators of Mouse Intesti... -

Data from ChEMBL 36 via Core Engine