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Compound Detail

CHEMBL5570406

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COc1cncc(C#Cc2cc(C(=O)Nc3ccc4c(c3)C(F)(F)C[C@@H]4N3CCN(C)CC3)ccc2F)c1

Basic Information

ChEMBL ID CHEMBL5570406
Phase Preclinical
Structure Type MOL
InChI Key KWCUYDDWUFSZAY-MHZLTWQESA-N
9
Targets
9
Activities
1
Assay Types
13
PK Parameters
16
Publications
0
Known Names

Molecular Properties

520.6
MW (Da)
4.67
ALogP
5
HBA
1
HBD
57.7
PSA (Ų)
0.51
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H27F3N4O2
MW 520.56
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.13

Activity Summary

IC50 9 meas. best 7.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 7.79 7.79 16.1 1
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 7.62 7.62 24.2 1
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 7.17 7.17 68.0 1
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 7.11 7.11 78.0 1
Cytochrome P450 3A4/3A5
CHEMBL2111472
IC50 5.42 5.42 3800.0 1
Cytochrome P450 2C19
CHEMBL3622
IC50 5.03 5.03 9400.0 1
Cytochrome P450 2C9
CHEMBL3397
IC50 5.01 5.01 9800.0 1
Cytochrome P450 2D6
CHEMBL289
IC50 4.9 4.9 12700.0 1
Cytochrome P450 1A2
CHEMBL3356
IC50 4.42 4.42 38400.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 3080.0 ng.hr.mL-1 Mus musculus
AUC 3144.0 ng.hr.mL-1 Mus musculus
AUC 623.0 ng.hr.mL-1 Mus musculus
AUC 656.0 ng.hr.mL-1 Mus musculus
CL 25.68 mL.min-1.kg-1 Mus musculus
Cmax 0.224 ug.mL-1 Mus musculus
F 47.9 % Mus musculus
MRT 9.67 hr Mus musculus
MRT 7.31 hr Mus musculus
T1/2 6.03 hr Mus musculus
T1/2 5.64 hr Mus musculus
Tmax 4.0 hr Mus musculus
Vd 12.42 L.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38294952 10.1021/acs.jmedchem.3c02040 ADMET 17
38294952 10.1021/acs.jmedchem.3c02040 Fibroblast growth factor receptor 2 5
38294952 10.1021/acs.jmedchem.3c02040 MFE-296 3
38294952 10.1021/acs.jmedchem.3c02040 Fibroblast growth factor receptor 1 3
38294952 10.1021/acs.jmedchem.3c02040 Fibroblast growth factor receptor 3 2
38294952 10.1021/acs.jmedchem.3c02040 Fibroblast growth factor receptor 4 2
38294952 10.1021/acs.jmedchem.3c02040 NCI-H716 1
38294952 10.1021/acs.jmedchem.3c02040 KATO III stomach cancer cell line 1
38294952 10.1021/acs.jmedchem.3c02040 KG-1a 1
38294952 10.1021/acs.jmedchem.3c02040 KMS-11 1
38294952 10.1021/acs.jmedchem.3c02040 MDA-MB-453 1
38294952 10.1021/acs.jmedchem.3c02040 Cytochrome P450 1A2 1
38294952 10.1021/acs.jmedchem.3c02040 Cytochrome P450 2C9 1
38294952 10.1021/acs.jmedchem.3c02040 Cytochrome P450 2C19 1
38294952 10.1021/acs.jmedchem.3c02040 Cytochrome P450 2D6 1
38294952 10.1021/acs.jmedchem.3c02040 Cytochrome P450 3A4/3A5 1

Data from ChEMBL 36 via Core Engine