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Compound Detail

CHEMBL601543

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CCN1/C(=C/C=C/c2oc3ccc(-c4ccccc4)cc3[n+]2CC)Oc2ccc(-c3ccccc3)cc21.CCOS(=O)(=O)[O-]

Basic Information

ChEMBL ID CHEMBL601543
Phase Preclinical
Structure Type MOL
InChI Key NSPWDHRUHGREHB-UHFFFAOYSA-M
Parent Compound CHEMBL585591
Active Moiety CHEMBL585591
13
Targets
29
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

485.6
MW (Da)
7.85
ALogP
3
HBA
0
HBD
29.5
PSA (Ų)
0.23
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H34N2O6S
MW 610.73
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -0.23

Activity Summary

EC50 22 meas. best 6.23
IC50 7 meas. best 5.84

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
ATP-dependent molecular chaperone HSP82
CHEMBL1293251
EC50 6.23 5.3467 589.0 3
Unchecked
CHEMBL612545
EC50 6.18 5.9817 659.0 6
BJ
CHEMBL614358
EC50 5.88 5.71 1320.0 3
CHO
CHEMBL613853
IC50 5.84 5.84 1448.0 1
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.82 5.82 1502.0 1
Alkaline phosphatase, tissue-nonspecific isozyme
CHEMBL5979
EC50 5.71 5.245 1930.0 4
Streptokinase A
CHEMBL1293228
EC50 5.68 5.68 2071.0 1
Unchecked
CHEMBL612545
IC50 5.43 5.335 3740.0 2
Streptococcus
CHEMBL612313
EC50 5.41 5.41 3887.0 1
NACHT, LRR and PYD domains-containing protein 3
CHEMBL1741208
IC50 5.05 5.045 8930.0 2
Beta Lactamase
CHEMBL1293246
IC50 4.97 4.97 10706.0 1
Toll-like receptor 9
CHEMBL5804
IC50 4.85 4.85 14137.0 1
Intestinal-type alkaline phosphatase
CHEMBL5573
EC50 4.62 4.62 24200.0 1
Alkaline phosphatase, germ cell type
CHEMBL3402
EC50 4.61 4.61 24500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
ATP-dependent molecular chaperone HSP82 EC50 = 589.0 nM 6.23 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay to Identify Inhibitors... -
Unchecked EC50 = 659.0 nM 6.18 PUBCHEM_BIOASSAY: Luminescence Cell-Based HTS Dose Confirmation to Identify Inhi... -
Unchecked EC50 = 696.0 nM 6.16 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response to Identify Inhibitors o... -
Unchecked EC50 = 863.0 nM 6.06 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response to Identify Inhibitors o... -
Unchecked EC50 = 976.0 nM 6.01 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Retest of Candida albicans Growth in t... -
Unchecked EC50 = 1045.0 nM 5.98 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
BJ EC50 = 1320.0 nM 5.88 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Comp... -
CHO IC50 = 1448.0 nM 5.84 PUBCHEM_BIOASSAY: Counterscreen for inhibitors of TLR9-MyD88 binding: Luminescen... -
Streptococcus sp. 'group A' EC50 = 1502.0 nM 5.82 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
BJ EC50 = 1629.0 nM 5.79 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Alkaline phosphatase, tissue-nonspecific isozyme EC50 = 1930.0 nM 5.71 PUBCHEM_BIOASSAY: SAR assay for compounds activating TNAP in the presence of 100... -
Streptokinase A EC50 = 2071.0 nM 5.68 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Unchecked EC50 = 3159.0 nM 5.5 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay for toxicity in mammal... -
Alkaline phosphatase, tissue-nonspecific isozyme EC50 = 3300.0 nM 5.48 PUBCHEM_BIOASSAY: SAR assay for compounds activating TNAP in the absence of phos... -
BJ EC50 = 3425.0 nM 5.46 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked IC50 = 3740.0 nM 5.43 PUBCHEM_BIOASSAY: High Throughput Screening Assay used to Identify Novel Compoun... -
Streptococcus EC50 = 3887.0 nM 5.41 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Alkaline phosphatase, tissue-nonspecific isozyme EC50 = 5144.5 nM 5.29 PUBCHEM_BIOASSAY: uHTS identification of compounds activating TNAP in the absenc... -
Unchecked IC50 = 5810.0 nM 5.24 PUBCHEM_BIOASSAY: A High Throughput Confirmatory Assay used to Identify Novel Co... -
ATP-dependent molecular chaperone HSP82 EC50 = 6544.0 nM 5.18 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay to Measure Toxicity of... -

Data from ChEMBL 36 via Core Engine