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Compound Detail

CHEMBL3809489

BEMCENTINIB
🧪 Phase II
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🧪 Phase II
Nc1nc(Nc2ccc3c(c2)CC[C@@H](N2CCCC2)CC3)nn1-c1cc2c(nn1)-c1ccccc1CCC2

Basic Information

ChEMBL ID CHEMBL3809489
Name BEMCENTINIB
Phase Phase II
Structure Type MOL
InChI Key KXMZDGSRSGHMMK-VWLOTQADSA-N

Known Names

Bemcentinib BGB 324 BGB-324 BGB324 CS-1046 HY-15150 KB-80319 QC-11751 R 428 R-428 R428 SYN-1131 +2 more
19
Targets
41
Activities
1
Assay Types
0
PK Parameters
20
Publications
14
Known Names
12
Indications
1
Mechanisms

Molecular Properties

506.7
MW (Da)
4.88
ALogP
8
HBA
2
HBD
97.8
PSA (Ų)
0.38
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer

Flags

Natural Product
USAN Stem -tinib
USAN Year 2018

Extended Properties

Molecular Formula C30H34N8
MW 506.66
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.08

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Tyrosine-protein kinase receptor UFO inhibitor INHIBITOR Tyrosine-protein kinase receptor UFO

Indications

Adenocarcinoma of Lung Carcinoma, Non-Small-Cell Lung Inflammatory Breast Neoplasms Mesothelioma Severe Acute Respiratory Syndrome Colorectal Neoplasms Leukemia, Myeloid, Acute Melanoma Myelodysplastic Syndromes Neoplasms Pancreatic Neoplasms Central Nervous System Neoplasms

Activity Summary

IC50 41 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase receptor UFO
CHEMBL4895
IC50 9.15 7.9671 0.7 17
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 9.05 8.6567 0.9 3
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
IC50 8.52 8.52 3.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 8.1 8.1 8.0 1
Tyrosine-protein kinase Mer
CHEMBL5331
IC50 7.82 6.7067 15.0 3
Tyrosine-protein kinase receptor TYRO3
CHEMBL5314
IC50 7.77 7.77 17.0 1
Platelet-derived growth factor receptor alpha
CHEMBL2007
IC50 7.7 7.7 20.0 1
Epithelial discoidin domain-containing receptor 1
CHEMBL5319
IC50 7.7 7.7 20.0 1
Aurora kinase A
CHEMBL4722
IC50 7.58 7.58 26.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 7.43 7.43 37.0 1
BaF3
CHEMBL614524
IC50 7.0 6.9533 98.8 3
Aurora kinase B
CHEMBL2185
IC50 7.0 7.0 100.0 1
Unchecked
CHEMBL612545
IC50 6.94 6.94 114.6 1
ALK tyrosine kinase receptor
CHEMBL4247
IC50 6.28 6.28 530.0 1
4T1
CHEMBL612589
IC50 6.03 6.03 940.0 1
Mast/stem cell growth factor receptor Kit
CHEMBL1936
IC50 6.0 6.0 1000.0 1
MDA-MB-231
CHEMBL400
IC50 5.55 5.55 2840.0 1
Hepatocyte growth factor receptor
CHEMBL3717
IC50 5.47 5.47 3400.0 1
Epidermal growth factor receptor
CHEMBL203
IC50 5.41 5.41 3900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase receptor UFO IC50 = 0.7 nM 9.15 Inhibition of wild-type human partial length AXL (R497 to Y821 residues) express... 29466002
Receptor-type tyrosine-protein kinase FLT3 IC50 = 0.9 nM 9.05 Inhibition of wild-type human partial length FLT3 (V592 to Y969 residues) expres... 29466002
Receptor-type tyrosine-protein kinase FLT3 IC50 = 2.0 nM 8.7 Inhibition of human partial length FLT3 D835Y mutant (Q580 to Y969 residues) exp... 29466002
Proto-oncogene tyrosine-protein kinase receptor Ret IC50 = 3.0 nM 8.52 Inhibition of wild-type human partial length RET (E713 to D1014 residues) expres... 29466002
Tyrosine-protein kinase receptor UFO IC50 = 3.3 nM 8.48 Inhibition of AXL (unknown origin) preincubated for 15 mins followed by substrat... 38913493
Tyrosine-protein kinase receptor UFO IC50 = 4.8 nM 8.32 Inhibition of AXL (unknown origin) using poly [Glu, Tyr] 4:1 as substrate incuba... 33733758
Tyrosine-protein kinase receptor UFO IC50 = 5.0 nM 8.3 Inhibition of human recombinant AXL incubated for 1 to 1.5 hrs by FRET based Z'-... 27379978
Tyrosine-protein kinase receptor UFO IC50 = 5.3 nM 8.28 Inhibition of AXL (unknown origin) by ELISA 33957388
Receptor-type tyrosine-protein kinase FLT3 IC50 = 6.0 nM 8.22 Inhibition of human partial length FLT3 ITD mutant expressed in bacterial expres... 29466002
Vascular endothelial growth factor receptor 2 IC50 = 8.0 nM 8.1 Inhibition of wild-type human partial length VEGFR2 (R787 to P1253 residues) exp... 29466002
Tyrosine-protein kinase receptor UFO IC50 = 8.5 nM 8.07 Inhibition of AXL (unknown origin) by ELISA analysis 38128234
Tyrosine-protein kinase receptor UFO IC50 = 9.9 nM 8.0 Inhibition of AXL in human HeLa cells incubated for 1 hr by ELISA 36358010
Tyrosine-protein kinase receptor UFO IC50 = 14.0 nM 7.85 Inhibition of AXL (unknown origin) 38128234
Tyrosine-protein kinase receptor UFO IC50 = 14.0 nM 7.85 Inhibition of recombinant AXL (unknown origin) by fluorescence polarization assa... 38913493
Tyrosine-protein kinase receptor UFO IC50 = 14.0 nM 7.85 Inhibition of AXL (unknown origin) 38714043
Tyrosine-protein kinase receptor UFO IC50 = 14.0 nM 7.85 Inhibition of AXL (unknown origin) 33539089
Tyrosine-protein kinase receptor UFO IC50 = 14.0 nM 7.85 Inhibition of AXL (unknown origin) 36358010
Tyrosine-protein kinase receptor UFO IC50 = 14.0 nM 7.85 Inhibition of AXL (unknown origin) 33957388
Tyrosine-protein kinase receptor UFO IC50 = 14.0 nM 7.85 Inhibition of Axl (unknown origin) 27379978
Tyrosine-protein kinase receptor UFO IC50 = 14.0 nM 7.85 Inhibition of human recombinant AXL by fluorescence polarization assay 26555154

Literature References

PubMed DOI Target Context # Activities
35279611 10.1016/j.ejmech.2022.114253 ADMET 11
38913493 10.1021/acs.jmedchem.4c00400 Unchecked 6
26555154 10.1021/acs.jmedchem.5b01273 Unchecked 4
27379978 10.1021/acs.jmedchem.6b00608 Tyrosine-protein kinase receptor UFO 4
- 10.6019/CHEMBL4495565 SARS-CoV-2 4
- 10.6019/CHEMBL4651402 SARS-CoV-2 4
29466002 10.1021/acs.jmedchem.7b01605 Receptor-type tyrosine-protein kinase FLT3 3
26555154 10.1021/acs.jmedchem.5b01273 Tyrosine-protein kinase receptor UFO 2
35279611 10.1016/j.ejmech.2022.114253 MDA-MB-231 2
38913493 10.1021/acs.jmedchem.4c00400 MDA-MB-231 2
38913493 10.1021/acs.jmedchem.4c00400 Tyrosine-protein kinase receptor UFO 2
- 10.6019/CHEMBL4651402 Vero C1008 2
38913493 10.1021/acs.jmedchem.4c00400 Tyrosine-protein kinase Mer 2
33733758 10.1021/acs.jmedchem.0c02093 BaF3 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
36325401 10.1039/d2md00153e Unchecked 2
36358010 10.1021/acs.jmedchem.2c01346 Tyrosine-protein kinase receptor UFO 2
33957388 10.1016/j.ejmech.2021.113497 Tyrosine-protein kinase receptor UFO 2
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 2
38128234 10.1016/j.ejmech.2023.116045 Tyrosine-protein kinase receptor UFO 2

Data from ChEMBL 36 via Core Engine