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Compound Detail

CHEMBL1514790

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CC[C@@H](C)[C@H](CNC)NC[C@@H](Cc1cccc2ccccc12)NCCc1cccc(C(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL1514790
Phase Preclinical
Structure Type MOL
InChI Key ZFKQBJHCEJBGQT-RZLJKOCPSA-N
7
Targets
17
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

485.6
MW (Da)
5.83
ALogP
3
HBA
3
HBD
36.1
PSA (Ų)
0.29
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H38F3N3
MW 485.64
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.34

Activity Summary

IC50 9 meas. best 5.06
EC50 8 meas. best 5.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Streptokinase A
CHEMBL1293228
EC50 5.61 5.61 2445.0 1
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.32 5.32 4797.0 1
Unchecked
CHEMBL612545
EC50 5.23 5.145 5860.0 4
Insulin-degrading enzyme
CHEMBL1293287
EC50 5.19 5.19 6410.0 1
Streptococcus
CHEMBL612313
EC50 5.15 5.15 7119.0 1
HEK293
CHEMBL614818
IC50 5.06 5.06 8670.0 1
Unchecked
CHEMBL612545
IC50 4.73 4.5014 18760.0 7
Apoptotic protease-activating factor 1
CHEMBL1795093
IC50 4.36 4.36 44100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Streptokinase A EC50 = 2445.0 nM 5.61 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptococcus sp. 'group A' EC50 = 4797.0 nM 5.32 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Unchecked EC50 = 5860.0 nM 5.23 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Insulin-degrading enzyme EC50 = 6410.0 nM 5.19 PUBCHEM_BIOASSAY: Fluorescence polarization-based cell-based high throughput dos... -
Unchecked EC50 = 7000.0 nM 5.16 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Streptococcus EC50 = 7119.0 nM 5.15 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Unchecked EC50 = 7843.0 nM 5.11 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Unchecked EC50 = 8358.0 nM 5.08 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
HEK293 IC50 = 8670.0 nM 5.06 PUBCHEM_BIOASSAY: Counterscreen for activators of insulin-degrading enzyme (IDE)... -
Unchecked IC50 = 18760.0 nM 4.73 PUBCHEM_BIOASSAY: A counter screen for small molecule screen for inhibitors of t... -
Unchecked IC50 = 19850.0 nM 4.7 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -
Unchecked IC50 = 21835.0 nM 4.66 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -
Unchecked IC50 = 32320.0 nM 4.49 PUBCHEM_BIOASSAY: A Counter Screen to identiry small molecule screen for inhibit... -
Unchecked IC50 = 33180.0 nM 4.48 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -
Unchecked IC50 = 39920.0 nM 4.4 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -
Apoptotic protease-activating factor 1 IC50 = 44100.0 nM 4.36 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 in a Fluore... -
Unchecked IC50 = 89900.0 nM 4.05 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 using a LZ-... -

Data from ChEMBL 36 via Core Engine