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Compound Detail

CHEMBL47203

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CN1CCN([C@H]2CC[C@@H](n3cc(-c4ccc(Oc5ccccc5)cc4)c4c(N)ncnc43)CC2)CC1

Basic Information

ChEMBL ID CHEMBL47203
Phase Preclinical
Structure Type MOL
InChI Key FDVSOQRNTAPCHB-ZRZAMGCNSA-N
10
Targets
10
Activities
1
Assay Types
7
PK Parameters
20
Publications
0
Known Names

Molecular Properties

482.6
MW (Da)
5.20
ALogP
7
HBA
1
HBD
72.4
PSA (Ų)
0.42
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H34N6O
MW 482.63
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.62

Activity Summary

IC50 10 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase Lck
CHEMBL258
IC50 7.82 7.82 15.0 1
Tyrosine-protein kinase Lyn
CHEMBL3905
IC50 7.54 7.54 29.0 1
Tyrosine-protein kinase CSK
CHEMBL2634
IC50 7.39 7.39 41.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 7.38 7.38 42.0 1
Tyrosine-protein kinase Blk
CHEMBL2250
IC50 7.34 7.34 46.0 1
Tyrosine-protein kinase Fyn
CHEMBL1841
IC50 7.23 7.23 59.0 1
Homo sapiens
CHEMBL372
IC50 7.16 7.16 70.0 1
Angiopoietin-1 receptor
CHEMBL4128
IC50 6.6 6.6 250.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 5.92 5.92 1190.0 1
Jurkat
CHEMBL397
IC50 4.6 4.6 25000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 661.0 ng.hr.mL-1 Rattus norvegicus
CL 88.33 mL.min-1.kg-1 Rattus norvegicus
Cmax 113.0 nM Rattus norvegicus
F 54.0 % Rattus norvegicus
T1/2 14.3 hr Rattus norvegicus
Tmax 4.0 hr Rattus norvegicus
Vd 140.0 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5303304 U2OS 9
- 10.6019/CHEMBL5303304 HEK-293T 8
12039590 10.1016/s0960-894x(02)00195-6 Rattus norvegicus 7
- 10.6019/CHEMBL5303304 Fibroblast 6
12039590 10.1016/s0960-894x(02)00195-6 Hepatocyte growth factor receptor 1
12039590 10.1016/s0960-894x(02)00195-6 Homo sapiens 1
12039590 10.1016/s0960-894x(02)00195-6 Jurkat 1
12039590 10.1016/s0960-894x(02)00195-6 Platelet-derived growth factor receptor 1
12039590 10.1016/s0960-894x(02)00195-6 Cyclin-dependent kinase 1 1
12039590 10.1016/s0960-894x(02)00195-6 Protein kinase C (PKC) 1
12039590 10.1016/s0960-894x(02)00195-6 Insulin receptor 1
12039590 10.1016/s0960-894x(02)00195-6 Unchecked 1
12039590 10.1016/s0960-894x(02)00195-6 Tyrosine-protein kinase Lck 1
12039590 10.1016/s0960-894x(02)00195-6 Tyrosine-protein kinase ZAP-70 1
12039590 10.1016/s0960-894x(02)00195-6 Tyrosine-protein kinase Lyn 1
12039590 10.1016/s0960-894x(02)00195-6 Tyrosine-protein kinase Fyn 1
12039590 10.1016/s0960-894x(02)00195-6 Tyrosine-protein kinase CSK 1
12039590 10.1016/s0960-894x(02)00195-6 Tyrosine-protein kinase Blk 1
12039590 10.1016/s0960-894x(02)00195-6 Angiopoietin-1 receptor 1
12039590 10.1016/s0960-894x(02)00195-6 Vascular endothelial growth factor receptor 2 1

Data from ChEMBL 36 via Core Engine