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Compound Detail

CHEMBL4802051

RL2578
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C=CC(=O)Nc1ccc2[nH]c(=O)n(C3CCN(Cc4ccc(-c5ccc6c(c5)NC(=O)CO6)cc4)CC3)c2c1

Basic Information

ChEMBL ID CHEMBL4802051
Name RL2578
Phase Preclinical
Structure Type MOL
InChI Key DHRJWFCFMBINAK-UHFFFAOYSA-N
6
Targets
18
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

523.6
MW (Da)
4.29
ALogP
6
HBA
3
HBD
108.5
PSA (Ų)
0.33
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H29N5O4
MW 523.59
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.20

Activity Summary

IC50 11 meas. best 5.72
EC50 7 meas. best 5.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 5.72 5.1375 1900.0 4
Unchecked
CHEMBL612545
IC50 5.72 5.1833 1900.0 3
Unchecked
CHEMBL612545
EC50 5.46 5.27 3500.0 3
RAC-beta serine/threonine-protein kinase
CHEMBL2431
EC50 5.38 5.38 4200.0 1
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
EC50 5.38 5.38 4200.0 1
ZR-75-1
CHEMBL614393
EC50 5.38 5.38 4200.0 1
RAC-beta serine/threonine-protein kinase
CHEMBL2431
IC50 5.08 4.915 8300.0 2
AN3-CA
CHEMBL1075392
EC50 4.75 4.75 18000.0 1
RAC-gamma serine/threonine-protein kinase
CHEMBL4816
IC50 4.75 4.75 18000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 1900.0 nM 5.72 NanoBRET assay (AKT1) -
RAC-alpha serine/threonine-protein kinase IC50 = 1900.0 nM 5.72 Affinity On-target Cellular interaction: (NanoBRET assay (HEK293T cells)) EUB000... -
Unchecked EC50 = 3500.0 nM 5.46 NanoBRET assay (AKT1) -
ZR-75-1 EC50 = 4200.0 nM 5.38 CellTiter-Glo luminescent cell viability assay (CTG) with ZR-75-1 cells -
RAC-alpha serine/threonine-protein kinase EC50 = 4200.0 nM 5.38 Affinity Phenotypic Cellular interaction: (CellTiter-Glo luminescent cell viabil... -
RAC-beta serine/threonine-protein kinase EC50 = 4200.0 nM 5.38 Affinity Phenotypic Cellular interaction: (CellTiter-Glo luminescent cell viabil... -
Unchecked EC50 = 4800.0 nM 5.32 NanoBRET assay (AKT2) -
Unchecked IC50 = 8300.0 nM 5.08 NanoBRET assay (AKT2) -
RAC-beta serine/threonine-protein kinase IC50 = 8300.0 nM 5.08 Affinity On-target Cellular interaction: (NanoBRET assay (HEK293T cells)) EUB000... -
RAC-alpha serine/threonine-protein kinase IC50 = 9200.0 nM 5.04 Homogeneous Time Resolved Fluorescence (HTRF) assay (AKT1) -
RAC-alpha serine/threonine-protein kinase IC50 = 9200.0 nM 5.04 Affinity Biochemical interaction: (HTFR assay) EUB0001563a AKT1 -
Unchecked EC50 = 9300.0 nM 5.03 NanoBRET assay (AKT3) -
AN3-CA EC50 = 18000.0 nM 4.75 CellTiter-Glo luminescent cell viability assay (CTG) with AN3-CA cells -
Unchecked IC50 = 18000.0 nM 4.75 NanoBRET assay (AKT3) -
RAC-alpha serine/threonine-protein kinase IC50 = 18000.0 nM 4.75 Affinity Phenotypic Cellular interaction: (CellTiter-Glo luminescent cell viabil... -
RAC-beta serine/threonine-protein kinase IC50 = 18000.0 nM 4.75 Affinity Phenotypic Cellular interaction: (CellTiter-Glo luminescent cell viabil... -
RAC-gamma serine/threonine-protein kinase IC50 = 18000.0 nM 4.75 Affinity Phenotypic Cellular interaction: (CellTiter-Glo luminescent cell viabil... -
RAC-gamma serine/threonine-protein kinase IC50 = 18000.0 nM 4.75 Selectivity interaction (NanoBRET assay (HEK293T cells)) EUB0001563a AKT3 -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5303300 HEK-293T 304
- 10.6019/CHEMBL5303300 Fibroblast 304
- 10.6019/CHEMBL5303300 U2OS 304
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL5303304 Fibroblast 9
- 10.6019/CHEMBL5303304 HEK-293T 8
- 10.6019/CHEMBL5303304 U2OS 8
- 10.6019/CHEMBL4800730 Unchecked 6
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
- 10.6019/CHEMBL5444388 RAC-alpha serine/threonine-protein kinase 2
- 10.6019/CHEMBL5444388 RAC-beta serine/threonine-protein kinase 2
- 10.6019/CHEMBL5308504 Casein kinase I isoform delta 1
- 10.6019/CHEMBL5308504 Peregrin 1
- 10.6019/CHEMBL5308504 Aurora kinase A 1
- 10.6019/CHEMBL5308504 Mitogen-activated protein kinase 1 1
- 10.6019/CHEMBL5308504 Glycogen synthase kinase-3 beta 1
- 10.6019/CHEMBL5308504 Cyclin-dependent kinase 2 1
- 10.6019/CHEMBL4800730 RAC-alpha serine/threonine-protein kinase 1

Data from ChEMBL 36 via Core Engine