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Compound Detail

CHEMBL461579

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CC[n+]1c(/C=C/N(C)c2ccccc2)n(-c2ccccc2)c2ccc(-c3nc4ccccc4s3)cc21.[I-]

Basic Information

ChEMBL ID CHEMBL461579
Phase Preclinical
Structure Type MOL
InChI Key NAYRELMNTQSBIN-UHFFFAOYSA-M
Parent Compound CHEMBL1186409
Active Moiety CHEMBL1186409
9
Targets
34
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

487.6
MW (Da)
7.32
ALogP
4
HBA
0
HBD
24.9
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 C31H27IN4S
MW 614.56
Aromatic Rings 6
Heavy Atoms 36
NP-Likeness -1.17

Activity Summary

EC50 19 meas. best 6.47
IC50 15 meas. best 6.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 6.47 5.8563 337.0 8
BJ
CHEMBL614358
EC50 6.45 5.7875 355.0 4
Unchecked
CHEMBL612545
IC50 6.06 5.2318 870.0 11
ATP-dependent molecular chaperone HSP82
CHEMBL1293251
EC50 5.92 5.2333 1195.0 3
Jurkat
CHEMBL397
IC50 5.82 5.82 1530.0 1
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.49 5.49 3267.0 1
Streptokinase A
CHEMBL1293228
EC50 5.44 5.16 3606.0 2
Ubiquitin-conjugating enzyme E2 N
CHEMBL6089
IC50 5.13 5.07 7423.0 2
Streptococcus
CHEMBL612313
EC50 4.92 4.92 12047.0 1
Bcl-2-related protein A1
CHEMBL1293239
IC50 4.88 4.88 13200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 337.0 nM 6.47 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Retest of Candida albicans Growth in t... -
Unchecked EC50 = 350.0 nM 6.46 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
BJ EC50 = 355.0 nM 6.45 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Dose Response to Characterize Compound... -
Unchecked EC50 = 387.0 nM 6.41 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Unchecked EC50 = 440.0 nM 6.36 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Unchecked EC50 = 460.0 nM 6.34 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Unchecked IC50 = 870.0 nM 6.06 PUBCHEM_BIOASSAY: High Throughput Screening Assay used to Identify Novel Compoun... -
Unchecked IC50 = 1040.0 nM 5.98 PUBCHEM_BIOASSAY: Dose response counterscreen of uHTS chemical inhibitors of bot... -
Unchecked IC50 = 1130.0 nM 5.95 PUBCHEM_BIOASSAY: A High Throughput Confirmatory Assay used to Identify Novel Co... -
ATP-dependent molecular chaperone HSP82 EC50 = 1195.0 nM 5.92 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay to Identify Inhibitors... -
Jurkat IC50 = 1530.0 nM 5.82 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS of chemical inhibitors of b... -
BJ EC50 = 2486.0 nM 5.6 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
BJ EC50 = 2704.0 nM 5.57 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
BJ EC50 = 2927.0 nM 5.53 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Comp... -
Unchecked EC50 = 3032.0 nM 5.52 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Streptococcus sp. 'group A' EC50 = 3267.0 nM 5.49 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptokinase A EC50 = 3606.0 nM 5.44 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Unchecked IC50 = 3920.0 nM 5.41 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS chemical inhibitors of both... -
Unchecked EC50 = 5718.0 nM 5.24 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Unchecked IC50 = 5900.0 nM 5.23 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -

Data from ChEMBL 36 via Core Engine