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Compound Detail

CHEMBL1087720

TRIMETHYLAPIGENIN
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COc1ccc(-c2cc(=O)c3c(OC)cc(OC)cc3o2)cc1

Basic Information

ChEMBL ID CHEMBL1087720
Name TRIMETHYLAPIGENIN
Phase Preclinical
Structure Type MOL
InChI Key ZXJJBDHPUHUUHD-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
28
PK Parameters
17
Publications
0
Known Names

Molecular Properties

312.3
MW (Da)
3.49
ALogP
5
HBA
0
HBD
57.9
PSA (Ų)
0.74
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C18H16O5
MW 312.32
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness 0.63

Activity Summary

IC50 1 meas. best 5.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
ATP-dependent translocase ABCB1
CHEMBL4302
IC50 5.85 5.85 1400.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1.96 ug.hr/g Rattus norvegicus
AUC 2.5 ug.hr/g Rattus norvegicus
AUC 1.88 ug.hr/g Rattus norvegicus
AUC 3.01 ug.hr/g Rattus norvegicus
AUC 7.83 ug.hr/g Rattus norvegicus
AUC 275660.0 ng.hr.mL-1 Rattus norvegicus
AUC 6960.0 ng.hr.mL-1 Rattus norvegicus
CL 6.3 ml/hr Rattus norvegicus
CL 337.0 ml/hr Rattus norvegicus
Cmax 1.1 ug/g Rattus norvegicus
Cmax 1.43 ug/g Rattus norvegicus
Cmax 1.41 ug/g Rattus norvegicus
Cmax 1.64 ug/g Rattus norvegicus
Cmax 3.01 ug/g Rattus norvegicus
Cmax 2817.62 nM Rattus norvegicus
F 1.75 % Rattus norvegicus
ka 8.53 /hr Rattus norvegicus
Ke 0.32 /hr Rattus norvegicus
Ke 0.15 /hr Rattus norvegicus
T1/2 4.19 hr Rattus norvegicus
T1/2 5.04 hr Rattus norvegicus
Tmax 3.14 hr Rattus norvegicus
Tmax 3.43 hr Rattus norvegicus
Tmax 1.76 hr Rattus norvegicus
Tmax 3.43 hr Rattus norvegicus
Tmax 2.64 hr Rattus norvegicus
Tmax 0.85 hr Rattus norvegicus
Vd 2385.1 ml Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
ATP-dependent translocase ABCB1 IC50 = 1400.0 nM 5.85 TP_TRANSPORTER: drug resistance (vincristine) in AML-2/D100 cells 15240100

Literature References

Data from ChEMBL 36 via Core Engine