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Compound Detail

CHEMBL1546374

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Cc1ccc(-[n+]2c(-c3ccc(Br)cc3)cn3c2CCc2ccc4cccnc4c2-3)cc1.[Br-]

Basic Information

ChEMBL ID CHEMBL1546374
Phase Preclinical
Structure Type MOL
InChI Key RNPPZAGTOGYHEM-UHFFFAOYSA-M
Parent Compound CHEMBL1624511
Active Moiety CHEMBL1624511
7
Targets
18
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

467.4
MW (Da)
6.14
ALogP
2
HBA
0
HBD
21.7
PSA (Ų)
0.29
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H21Br2N3
MW 547.29
Aromatic Rings 5
Heavy Atoms 31
NP-Likeness -0.74

Activity Summary

IC50 10 meas. best 6.12
EC50 8 meas. best 6.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
BJ
CHEMBL614358
EC50 6.19 5.83 649.0 3
Unchecked
CHEMBL612545
EC50 6.12 5.79 760.0 2
Unchecked
CHEMBL612545
IC50 6.12 4.7117 760.0 6
Sphingosine 1-phosphate receptor 2
CHEMBL2955
IC50 5.83 5.6 1488.0 2
Streptokinase A
CHEMBL1293228
EC50 5.44 5.315 3602.0 2
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.19 5.19 6512.0 1
Exodeoxyribonuclease V
CHEMBL2095232
IC50 4.55 4.55 28433.0 1
Nuclear receptor subfamily 4immunitygroup A member 1
CHEMBL1293229
IC50 4.38 4.38 41371.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
BJ EC50 = 649.0 nM 6.19 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked EC50 = 760.0 nM 6.12 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Unchecked IC50 = 760.0 nM 6.12 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Inhibitors of Mycobacterium... -
Sphingosine 1-phosphate receptor 2 IC50 = 1488.0 nM 5.83 PUBCHEM_BIOASSAY: Counterscreen for S1P2 Antagonists: Dose Response Cell-Based S... -
BJ EC50 = 1689.0 nM 5.77 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Comp... -
BJ EC50 = 2979.0 nM 5.53 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked EC50 = 3507.0 nM 5.46 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Streptokinase A EC50 = 3602.0 nM 5.44 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Sphingosine 1-phosphate receptor 2 IC50 = 4278.0 nM 5.37 PUBCHEM_BIOASSAY: Dose Response Cell Based Assay for Antagonists of the S1P2 Rec... -
Streptococcus sp. 'group A' EC50 = 6512.0 nM 5.19 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptokinase A EC50 = 6498.0 nM 5.19 PUBCHEM_BIOASSAY: Absorbance Microorganism-Based Dose Response HTS to Identify I... -
Unchecked IC50 = 17127.0 nM 4.77 PUBCHEM_BIOASSAY: Absorbance-based bacterial cell-based high throughput dose res... -
Unchecked IC50 = 16854.0 nM 4.77 PUBCHEM_BIOASSAY: Counterscreen for AddAB inhibitors: absorbance-based bacterial... -
Exodeoxyribonuclease V IC50 = 28433.0 nM 4.55 PUBCHEM_BIOASSAY: Counterscreen for AddAB inhibitors: absorbance-based bacterial... -
Unchecked IC50 = 40600.0 nM 4.39 PUBCHEM_BIOASSAY: A counter screen for small molecule screen for inhibitors of t... -
Nuclear receptor subfamily 4immunitygroup A member 1 IC50 = 41371.0 nM 4.38 PUBCHEM_BIOASSAY: High Throughput Fluorescence Polarization Screen for Bcl-B Phe... -
Unchecked IC50 = 62240.0 nM 4.21 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -
Unchecked IC50 = 97544.0 nM 4.01 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -

Data from ChEMBL 36 via Core Engine