Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL4448899

BAY-876
Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
Cc1c(NC(=O)c2cc(C(N)=O)nc3cc(F)ccc23)c(C(F)(F)F)nn1Cc1ccc(C#N)cc1

Basic Information

ChEMBL ID CHEMBL4448899
Name BAY-876
Phase Preclinical
Structure Type MOL
InChI Key BKLJDIJJOOQUFG-UHFFFAOYSA-N
11
Targets
37
Activities
2
Assay Types
16
PK Parameters
20
Publications
0
Known Names

Molecular Properties

496.4
MW (Da)
4.17
ALogP
6
HBA
2
HBD
126.7
PSA (Ų)
0.40
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug Chemical Probe

Extended Properties

Molecular Formula C24H16F4N6O2
MW 496.42
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.89

Activity Summary

IC50 32 meas. best 8.7
Ki 5 meas. best 5.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Solute carrier family 2, facilitated glucose transporter member 1
CHEMBL2535
IC50 8.7 7.998 2.0 15
OVCAR-3
CHEMBL614213
IC50 7.22 7.22 60.0 1
SK-OV-3
CHEMBL614925
IC50 6.73 6.73 188.0 1
Solute carrier family 2, facilitated glucose transporter member 4
CHEMBL5874
IC50 6.7 6.328 200.0 5
HEY
CHEMBL613869
IC50 6.0 6.0 1002.0 1
Prostaglandin E2 receptor EP4 subtype
CHEMBL1836
IC50 5.95 5.95 1120.0 1
Adenosine receptor A3
CHEMBL256
IC50 5.94 5.94 1140.0 1
Solute carrier family 2, facilitated glucose transporter member 3
CHEMBL5215
IC50 5.8 5.675 1600.0 4
Histamine H2 receptor
CHEMBL1941
Ki 5.1 5.0933 7943.3 3
Solute carrier family 2, facilitated glucose transporter member 2
CHEMBL5873
IC50 5.03 5.01 9400.0 3
Histamine H1 receptor
CHEMBL231
Ki 5.0 5.0 10000.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 7.667 mL.min-1.kg-1 Rattus norvegicus
CL 5.333 mL.min-1.kg-1 Homo sapiens
CL 5.5 mL.min-1.kg-1 Mus musculus
CL 12.67 mL.min-1.kg-1 Macaca mulatta
CL 18.33 mL.min-1.kg-1 Rattus norvegicus
CL 3.333 mL.min-1.kg-1 Canis lupus familiaris
CL 6.167 mL.min-1.kg-1 Homo sapiens
CL 23.33 mL.min-1.kg-1 Macaca mulatta
CL 3.833 mL.min-1.kg-1 Rattus norvegicus
CL 5.5 mL.min-1.kg-1 Rattus norvegicus
CL 0.55 mL.min-1.kg-1 Canis lupus familiaris
CL 0.9833 mL.min-1.kg-1 Canis lupus familiaris
F 85.0 % Rattus norvegicus
F 79.0 % Canis lupus familiaris
T1/2 2.5 hr Rattus norvegicus
T1/2 22.0 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 2.0 nM 8.7 Cell-based assay with CellTiter-Glo readout for ATP production with SLC2A1 -
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 2.0 nM 8.7 Inhibition of human GLUT1 expressed in DLD1 cells assessed as glucose uptake by ... 31774679
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 2.0 nM 8.7 Inhibition of human GLUT1 expressed in CHO-K1 cells constitutively expressing lu... 31344028
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 2.0 nM 8.7 Inhibition of human GLUT1 expressed in human DLD-1 cells assessed as reduction i... 27552707
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 2.0 nM 8.7 Affinity On-target Cellular interaction (CellTiter-Glo® Luminescent Cell Viabili... -
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 3.2 nM 8.49 Cellular mechanistic assay: Inhibition of glucose uptake by Hela-MaTu cells -
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 3.2 nM 8.49 Affinity Phenotypic Cellular interaction (Cellular mechanistic assay (inhibition... -
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 25.0 nM 7.6 Inhibition of GLUT1 in human SK-OV-3 cells assessed as decrease in conversion of... 30602670
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 25.0 nM 7.6 Inhibition of GLUT1 in human OVCAR-3 cells assessed as decrease in conversion of... 30602670
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 25.0 nM 7.6 Inhibition of GLUT1 in human HEY cells assessed as decrease in conversion of D-[... 30602670
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 25.0 nM 7.6 Inhibition of GLUT1 in human OVCR-429 cells assessed as decrease in conversion o... 30602670
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 25.0 nM 7.6 Inhibition of GLUT1 in human OVCA-432 cells assessed as decrease in conversion o... 30602670
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 27.0 nM 7.57 Selectivity interaction (Proliferation assay (HelaMa TU cells)) EUB0000307b SLC2... -
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 50.0 nM 7.3 Inhibition of GLUT1 in human wild-type DLD1 cells assessed as reduction in ATP l... 32282207
OVCAR-3 IC50 = 60.0 nM 7.22 Antiproliferative activity against human OVCAR-3 cells assessed as reduction in ... 30602670
SK-OV-3 IC50 = 188.0 nM 6.73 Antiproliferative activity against human SK-OV-3 cells assessed as reduction in ... 30602670
Solute carrier family 2, facilitated glucose transporter member 4 IC50 = 200.0 nM 6.7 Inhibition of human GLUT4 expressed in CHO cells measured after 15 mins by cell-... 31344028
Solute carrier family 2, facilitated glucose transporter member 1 IC50 = 240.0 nM 6.62 Inhibition of the Glucose Transporter (GLUT1, SLC2A1) as assessed by a FRET base... -
Solute carrier family 2, facilitated glucose transporter member 4 IC50 = 270.0 nM 6.57 Cell-based assay with CellTiter-Glo readout for ATP production with SLC2A4 -
Solute carrier family 2, facilitated glucose transporter member 4 IC50 = 270.0 nM 6.57 Selectivity interaction (Glucose transporter panel CellTiter-Glo® Luminescent Ce... -

Literature References

PubMed DOI Target Context # Activities
30602670 10.3390/cancers11010033 Solute carrier family 2, facilitated glucose transporter member 1 40
27552707 10.1002/cmdc.201600276 ADMET 32
32404031 10.1161/circresaha.119.316463 Solute carrier family 2, facilitated glucose transporter member 1 23
- 10.6019/CHEMBL4507267 Tyrosine-protein kinase ABL1 15
- 10.6019/CHEMBL4507267 Epidermal growth factor receptor 12
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL4507267 Receptor-type tyrosine-protein kinase FLT3 11
- 10.6019/CHEMBL4689842 U2OS 10
- 10.6019/CHEMBL4507267 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 10
- 10.6019/CHEMBL4689842 HEK-293T 9
- 10.6019/CHEMBL4689842 Fibroblast 9
- 10.6019/CHEMBL4507267 Mast/stem cell growth factor receptor Kit 9
- 10.6019/CHEMBL4507267 Unchecked 8
30602670 10.3390/cancers11010033 SK-OV-3 7
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
31344028 10.1371/journal.pone.0217885 Solute carrier family 2, facilitated glucose transporter member 1 5
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
30602670 10.3390/cancers11010033 OVCAR-3 5
- 10.6019/CHEMBL4507267 Proto-oncogene tyrosine-protein kinase receptor Ret 4

Data from ChEMBL 36 via Core Engine