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Compound Detail

CHEMBL4555711

BAY-9897
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COc1cc(N[C@@H]2CCCC[C@]2(O)C(F)(F)F)ccc1F

Basic Information

ChEMBL ID CHEMBL4555711
Name BAY-9897
Phase Preclinical
Structure Type MOL
InChI Key CWRARANSONEPBZ-CHWSQXEVSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

307.3
MW (Da)
3.48
ALogP
3
HBA
2
HBD
41.5
PSA (Ų)
0.84
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H17F4NO2
MW 307.29
Aromatic Rings 1
Heavy Atoms 21
NP-Likeness -0.32

Activity Summary

Ki 2 meas. best 5.01
IC50 1 meas. best 5.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H2 receptor
CHEMBL1941
Ki 5.01 5.01 9772.4 2
Short transient receptor potential channel 5
CHEMBL1250411
IC50 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H2 receptor Ki = 9781.38 nM 5.01 GPCRScan assay: inhibition of H2 -
Histamine H2 receptor Ki = 9772.37 nM 5.01 GPCRScan assay: inhibition of H2 -
Short transient receptor potential channel 5 IC50 = 10000.0 nM 5.0 TRP selectivity screen (TRPC5) -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL5303304 U2OS 7
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
- 10.6019/CHEMBL5303304 HEK-293T 4
- 10.6019/CHEMBL4507328 Histamine H2 receptor 3
- 10.6019/CHEMBL4507328 GABA-A receptor; anion channel 2
36622903 10.1021/acs.jmedchem.2c01830 Transient receptor potential cation channel subfamily A member 1 2
- 10.6019/CHEMBL4507328 Transient receptor potential cation channel subfamily A member 1 2
- 10.6019/CHEMBL4507328 Histamine H1 receptor 1
- 10.1021/acschembio.2c00877 Colon organoid 1
- 10.6019/CHEMBL4507328 Muscarinic acetylcholine receptor M2 1
- 10.6019/CHEMBL4507328 Muscarinic acetylcholine receptor M1 1
- 10.6019/CHEMBL4507328 Histamine H3 receptor 1
- 10.6019/CHEMBL4507328 Beta-2 adrenergic receptor 1
- 10.6019/CHEMBL4507328 5-hydroxytryptamine receptor 5A 1
- 10.6019/CHEMBL4507328 5-hydroxytryptamine receptor 2C 1
- 10.6019/CHEMBL4507328 Short transient receptor potential channel 6 1
- 10.6019/CHEMBL4507328 Transient receptor potential cation channel subfamily V member 4 1

Data from ChEMBL 36 via Core Engine