| Tyrosyl-DNA phosphodiesterase 1 |
Potency |
= |
70794.6 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors of Tyrosyl-DNA Phosphodiesterase (TDP1). (Class of assay: confirmatory) |
CHEMBL1201862 |
| Hepatotoxicity |
Hepatotoxicity |
|
|
|
Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans |
CHEMBL1697731 |
| Hepatotoxicity |
Hepatotoxicity |
|
|
|
Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents |
CHEMBL1697731 |
| Hepatotoxicity |
Hepatotoxicity |
|
|
|
Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents |
CHEMBL1697731 |
| Unchecked |
Potency |
|
104903.6 |
nM |
PubChem BioAssay. Cell Proliferation Assay against the HBL1 Cell Line. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Unchecked |
Potency |
|
0.005258 |
nM |
PubChem BioAssay. Cell Proliferation Assay against the TMD8 Cell Line. (Class of assay: confirmatory) |
CHEMBL1201862 |
| HEL |
MCC |
> |
100000.0 |
nM |
Cytotoxicity against HEL cells |
CHEMBL3085645 |
| Felid herpesvirus 1 |
EC50 |
> |
100000.0 |
nM |
Antiviral activity against Feline herpesvirus infected in cat CRFK cells assessed as inhibition of virus-induced cytopathicity |
CHEMBL3085645 |
| Human herpesvirus 1 strain KOS |
EC50 |
> |
100000.0 |
nM |
Antiviral activity against acyclovir-resistant thymidine kinase-deficient Herpes simplex virus 1 KOS infected in HEL cells assessed as inhibition of virus-induced cytopathicity |
CHEMBL3085645 |
| Human herpesvirus 2 strain G |
EC50 |
> |
100000.0 |
nM |
Antiviral activity against Herpes simplex virus 2 G infected in HEL cells assessed as inhibition of virus-induced cytopathicity |
CHEMBL3085645 |
| Human herpesvirus 1 strain KOS |
EC50 |
> |
100000.0 |
nM |
Antiviral activity against Herpes simplex virus 1 KOS infected in HEL cells assessed as inhibition of virus-induced cytopathicity |
CHEMBL3085645 |
| HeLa |
IC50 |
>= |
250000.0 |
nM |
Cytostatic activity against thymidine kinase-deficient human HeLa cells assessed as growth inhibition after 3 days by particle counting analysis |
CHEMBL3085645 |
| HeLa |
IC50 |
= |
165000.0 |
nM |
Cytostatic activity against human HeLa cells assessed as growth inhibition after 3 days by particle counting analysis |
CHEMBL3085645 |
| CEM |
IC50 |
= |
210000.0 |
nM |
Cytostatic activity against human CEM cells assessed as growth inhibition after 3 days by particle counting analysis |
CHEMBL3085645 |
| L1210 |
IC50 |
>= |
250000.0 |
nM |
Cytostatic activity against mouse L1210 cells assessed as growth inhibition after 2 days by particle counting analysis |
CHEMBL3085645 |
| Unchecked |
Potency |
|
33173.4 |
nM |
PubChem BioAssay. Cell Proliferation Assay Versus the ED40515 IL2 Dependent ATL cell lines. (Class of assay: confirmatory) |
CHEMBL1201862 |
| NON-PROTEIN TARGET |
Potency |
|
4.2 |
nM |
PubChem BioAssay. qHTS profiling for inhibitors of Plasmodium falciparum (3D7) proliferation. (Class of assay: confirmatory) |
CHEMBL1201862 |
| NON-PROTEIN TARGET |
Potency |
|
9.4 |
nM |
PubChem BioAssay. qHTS profiling for inhibitors of Plasmodium falciparum (HB3) proliferation. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Unchecked |
Potency |
|
661.9 |
nM |
PubChem BioAssay. Cell Proliferation Assay Versus the ED40515 IL2 Independent ATL cell lines. (Class of assay: confirmatory) |
CHEMBL1201862 |
| NON-PROTEIN TARGET |
Potency |
|
0.8 |
nM |
PubChem BioAssay. qHTS profiling for inhibitors of Plasmodium falciparum (DD2) proliferation. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Mus musculus |
Activity |
|
|
|
Activation of AMPK in C57BL/6J mouse skeletal muscle assessed as increase of PGC-1alpha transcription at 500 mg/kg, sc after 2 hrs by Western blot analysis |
CHEMBL3286138 |
| Unchecked |
Activity |
|
|
|
Activation of AMPK in mouse 3T3L1 cells assessed as AMPK phosphorylation at 500 uM after 5 hrs by Western blotting analysis |
CHEMBL3352398 |
| 3T3-L1 |
Inhibition |
= |
50.96 |
% |
Inhibition of triglyceride accumulation in mouse 3T3L1 cells at 10 uM after 24 hrs |
CHEMBL3352801 |
| Unchecked |
AC50 |
|
7079.5 |
nM |
PubChem BioAssay. qHTS Assay for Identifying Compounds that block Entry of Ebola Virus, Screen 2 green channel. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Unchecked |
Ac50 |
|
1.259 |
uM |
PubChem BioAssay. qHTS Assay for Identifying Compounds that block Entry of Ebola Virus: Screen 2, blue channel. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Unchecked |
Potency |
|
1662.6 |
nM |
PubChem BioAssay. Immunotoxin (HA22) sensitization/mitigation study - treatment arm (High Dose). (Class of assay: confirmatory) |
CHEMBL1201862 |
| Unchecked |
Ac50 |
|
7.079 |
uM |
PubChem BioAssay. qHTS Assay for Identifying Compounds that block Entry of Ebola Virus: Screen 2, green channel. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Unchecked |
AC50 |
|
1258.9 |
nM |
PubChem BioAssay. qHTS Assay for Identifying Compounds that block Entry of Ebola Virus, Screen 2 blue channel. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Molecular identity unknown |
Activity |
|
|
|
Reduction in FAS protein expression in mouse 3T3L1 cells at 0.2 mM after 3 days by Western blot method |
CHEMBL3596120 |
| Molecular identity unknown |
Activity |
|
|
|
Reduction in C/EBPalpha protein expression in mouse 3T3L1 cells at 0.2 mM after 3 days by Western blot method |
CHEMBL3596120 |
| Molecular identity unknown |
Activity |
|
|
|
Reduction in PPARgamma protein expression in mouse 3T3L1 cells at 0.2 mM after 3 days by Western blot method |
CHEMBL3596120 |
| Molecular identity unknown |
Activity |
|
|
|
Reduction in SREBP-1c protein expression in mouse 3T3L1 cells at 0.2 mM after 3 days by Western blot method |
CHEMBL3596120 |
| Molecular identity unknown |
Activity |
|
|
|
Reduction in SCD1 protein expression in mouse 3T3L1 cells at 0.2 mM after 3 days by Western blot method |
CHEMBL3596120 |
| Unchecked |
Activity |
|
|
|
Activation of AMPK in mouse 3T3L1 cells assessed as increase in ACC Ser79 phosphorylation at 0.2 mM after 9 days by Western blot method |
CHEMBL3596120 |
| Unchecked |
Activity |
|
|
|
Increase in AMPKalpha Thr172 phosphorylation in mouse 3T3L1 cells at 0.2 mM after 9 days by Western blot method |
CHEMBL3596120 |
| 3T3-L1 |
Activity |
|
|
|
Inhibition of adipogenesis in mouse 3T3L1 cells assessed as reduction in triglyceride content at 0.2 mM by colorimetric assay |
CHEMBL3596120 |
| 3T3-L1 |
Activity |
|
|
|
Effect on in AMPKalpha protein expression in mouse 3T3L1 cells at 25 uM after 0.5 to 4 hrs by Western blot method |
CHEMBL3596120 |
| Unchecked |
Activity |
|
|
|
Activation of AMPK in mouse C2C12 cells assessed as increase in ACC phosphorylation at Ser79 residues at 1 mM after 1 hr by Western blot analysis |
CHEMBL3871291 |
| K562 |
IC50 |
= |
800000.0 |
nM |
Antileukemic activity against human K562 cells after 48 hrs by XTT assay |
CHEMBL4004814 |
| Protein-tyrosine phosphatase 1B |
Inhibition |
|
|
% |
Inhibition of PTP1B in differentiated mouse C2C12 cells assessed as upregulation of ACC phosphorylation at Ser-79 residue at 0.2 mM after 30 mins by Western blot assay |
CHEMBL4043257 |
| RCC4 |
IC50 |
= |
250000.0 |
nM |
Anticancer activity against human RCC4 cells after 48 hrs by XTT assay |
CHEMBL4049416 |
| MDA-MB-231 |
IC50 |
= |
1000000.0 |
nM |
Anticancer activity against human MDA-MB-231 cells after 48 hrs by XTT assay |
CHEMBL4049416 |
| RCC4 |
Activity |
|
|
|
Induction of autophagy in human RCC4 cells assessed as increase in LC3 conversion at 1 mM after 48 hrs by Western blot method |
CHEMBL4049416 |
| K-562R |
IC50 |
= |
800000.0 |
nM |
Cytotoxicity in imatinib-resistant human K562R cells assessed as reduction cell viability incubated for 48 hrs by XTT assay |
CHEMBL4118130 |
| K562 |
IC50 |
= |
800000.0 |
nM |
Cytotoxicity in drug sensitive human K562 cells assessed as reduction cell viability incubated for 48 hrs by XTT assay |
CHEMBL4118130 |
| Unchecked |
Activity |
|
|
|
Induction of AMPKalpha phosphorylation at Thr172 residue in mouse 3T3L1 cells at 2 mM after 4 hrs by Western blot analysis |
CHEMBL4145536 |
| SARS-CoV-2 |
Inhibition |
= |
-4.27 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging |
CHEMBL4303101 |
| Glycogen synthase kinase-3 |
FC |
= |
2.0 |
|
Activation of GSK3 phosphorylation in human HepG2 cells at MNTD after 18 hrs by Western blot analysis relative to control |
CHEMBL4411265 |
| Replicase polyprotein 1ab |
Inhibition |
= |
7.481 |
% |
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate |
CHEMBL4495564 |
| SARS-CoV-2 |
Inhibition |
= |
-0.07 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
| AMP-activated protein kinase, AMPK |
EC50 |
|
|
|
Activation of AMPK in human MDA-MB-435 cells measured after 2 hrs by anti-phospho-Acetyl-CoA Carboxylase (Ser79) antibody-based ELISA |
CHEMBL4627268 |
| MDA-MB-453 |
IC50 |
= |
1700000.0 |
nM |
Antiproliferation activity against human MDA-MB-453 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay |
CHEMBL4627268 |
| SK-BR-3 |
IC50 |
= |
180000.0 |
nM |
Antiproliferation activity against human SK-BR-3 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay |
CHEMBL4627268 |
| No relevant target |
solubility |
|
|
|
Aqueous solubility of the compound in pH 1.2 JP1 fluid incubated for 20 hrs by liquid chromatography |
CHEMBL4627268 |
| No relevant target |
solubility |
|
|
|
Aqueous solubility of the compound in pH 6.8 JP2 fluid incubated for 20 hrs by liquid chromatography |
CHEMBL4627268 |
| No relevant target |
solubility |
|
|
|
Aqueous solubility of the compound in pH 6.8 JP2 fluid incubated for 20 hrs in presence of taurocholic acid by liquid chromatography |
CHEMBL4627268 |
| SARS-CoV-2 |
Inhibition |
= |
-0.07 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
| SARS-CoV-2 |
IC50 |
> |
20000.0 |
nM |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4651402 |
| SARS-CoV-2 |
IC50 |
< |
19952.62 |
nM |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4651402 |
| MCF7 |
TGI |
= |
42.16 |
% |
Antitumor activity against human MCF7 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 200 mg/kg, ip administered every other day for 2 weeks relative to control |
CHEMBL4673179 |
| Unchecked |
Activity |
|
|
|
Activation of AMPK pathway in mouse 3T3-L1 cells assessed as increase in number of mitochondria copy at 2 uM after 24 hrs by mito-tracker staining based Confocal microscopic method |
CHEMBL4732044 |
| Unchecked |
Activity |
|
|
|
Activation of AMPK pathway in mouse 3T3-L1 cells assessed as increase in number of mitochondria copy at 2 uM after 24 hrs in presence of compound C by mito-tracker staining based Confocal microscopic method |
CHEMBL4732044 |
| Unchecked |
Activity |
|
|
|
Activation of AMPK in oleic, palmitic, linoleic and arachidonic acid 29:47:18:6 (v/v)-induced human HepG2 cells assessed as increase in AMPK phosphorylation by Western blot |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
Activation of AMPK in oleic, palmitic, linoleic and arachidonic acid 29:47:18:6 (v/v)-induced human HepG2 cells assessed as increase in ACC phosphorylation by Western blot |
CHEMBL4765421 |
| Mus musculus |
Activity |
|
|
|
Hypolipidemic activity in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as reduction in serum total cholesterol level at 100 mg/kg, po measured after 24 hrs |
CHEMBL4765421 |
| Mus musculus |
Activity |
|
|
|
Hypolipidemic activity in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as reduction in serum triglyceride level at 100 mg/kg, po measured after 24 hrs |
CHEMBL4765421 |
| Mus musculus |
Activity |
|
|
|
Hypolipidemic activity in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as reduction in serum LDL level at 100 mg/kg, po measured after 24 hrs |
CHEMBL4765421 |
| Mus musculus |
Activity |
|
|
|
Hypolipidemic activity in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as reduction in serum AST level at 100 mg/kg, po measured after 24 hrs |
CHEMBL4765421 |
| Mus musculus |
Activity |
|
|
|
Hypolipidemic activity in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as reduction in serum ALT level at 100 mg/kg, po measured after 24 hrs |
CHEMBL4765421 |
| Mus musculus |
Activity |
|
|
|
Hypolipidemic activity in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as reduction in serum IL6 level at 100 mg/kg, po measured after 24 hrs |
CHEMBL4765421 |
| Mus musculus |
Activity |
|
|
|
Hypolipidemic activity in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as reduction in fatty liver phenotype at 100 mg/kg, po measured after 24 hrs |
CHEMBL4765421 |
| Mus musculus |
Activity |
|
|
|
Hypolipidemic activity in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as reduction in lipid level in liver at 100 mg/kg, po measured after 24 hrs by Oil Red O staining based assay |
CHEMBL4765421 |
| Mus musculus |
Activity |
|
|
|
Hypolipidemic activity in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as increase in appearance of hepatic lobules at 100 mg/kg, po measured after 24 hrs by Oil Red O staining based assay |
CHEMBL4765421 |
| Mus musculus |
Activity_index |
= |
57.41 |
|
Hypolipidemic activity in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as liver index at 100 mg/kg, po measured after 24 hrs (Rvb = 65.00 +/- 0.87 No_unit) |
CHEMBL4765421 |
| Mus musculus |
Activity_index |
= |
8.64 |
|
Hypolipidemic activity in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as kidney index at 100 mg/kg, po measured after 24 hrs (Rvb = 11.20 +/- 0.58 No_unit) |
CHEMBL4765421 |
| Mus musculus |
Activity_index |
= |
3.01 |
|
Hypolipidemic activity in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as spleen index at 100 mg/kg, po measured after 24 hrs (Rvb = 3.87 +/- 0.05 No_unit) |
CHEMBL4765421 |
| Mus musculus |
Activity_index |
= |
15.94 |
|
Hypolipidemic activity in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as perirenal white adipose tissue index at 100 mg/kg, po measured after 24 hrs (Rvb = 18.14 +/- 1.44 No_unit) |
CHEMBL4765421 |
| Mus musculus |
Activity_index |
= |
20.09 |
|
Hypolipidemic activity in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as epididymis white adipose tissue index at 100 mg/kg, po measured after 24 hrs (Rvb = 23.43 +/- 3.10 No_unit) |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo induction of AMPK in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as increase in AKT phosphorylation in white adipose tissue at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo induction of AMPK in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as increase in AKT phosphorylation in liver at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo induction of AMPK in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as increase in AMPKalpha phosphorylation in white adipose tissue at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo induction of AMPK in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as increase in AMPKalpha phosphorylation in liver at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo induction of AMPK in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as increase in ACC phosphorylation in white adipose tissue at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo induction of AMPK in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as increase in ACC phosphorylation in liver at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo induction of AMPK in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as increase in CPT-1A phosphorylation in white adipose tissue at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo induction of AMPK in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as increase in CPT-1A phosphorylation in liver at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo induction of AMPK in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as decrease in SREBP1-C expression in white adipose tissue at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo induction of AMPK in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as decrease in SREBP1-C expression in liver at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo induction of AMPK in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as decrease in FAS expression in white adipose tissue at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo induction of AMPK in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as decrease in FAS expression in liver at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo effect on PPAR signaling in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as increase in mTOR phosphorylation in liver at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo effect on PPAR signaling in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as increase in mTOR phosphorylation in white adipose tissue at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo effect on PPAR signaling in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as increase in PPARalpha expression in white adipose tissue at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo effect on PPAR signaling in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as increase in PPARalpha expression in liver at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo effect on PPAR signaling in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as decrease in PPARbeta expression in white adipose tissue at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo effect on PPAR signaling in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as increase in PPARbeta expression in liver at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo effect on PPAR signaling in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as decrease in PPARgamma expression in white adipose tissue at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
In vivo effect on PPAR signaling in tyloxapol-induced Kunming mouse model of hyperlipidemia assessed as decrease in PPARgamma expression in liver at 100 mg/kg, po measured after 24 hrs by Western blot analysis |
CHEMBL4765421 |
| Unchecked |
Activity |
|
|
|
Effect on AMPK in mouse C2C12 myotubes assessed as increase in AMPK-alpha phosphorylation at Thr172 at 1 mM measured after 1 hrs by western blot analysis |
CHEMBL5046261 |
| Unchecked |
IC50 |
= |
5300.0 |
nM |
Cytotoxicity against paclitaxel-resistant human HCT116tax cells assessed as DNA damage by measuring fluorescence intensity incubated for 30 mins by Hoechst 33342 staining accumulation assay |
CHEMBL5104221 |
| HCT-116 |
Activity |
|
|
|
Cytotoxicity against human HCT-116 cells overexpressing human MDR1 assessed as DNA damage by measuring fluorescence intensity at 100 uM incubated for 30 mins by Hoechst 33342 staining accumulation assay |
CHEMBL5104221 |
| HCT-116 |
Activity |
|
|
|
Cytotoxicity against in human HCT-116 cells overexpressing human BCRP assessed as DNA damage by measuring fluorescence intensity at 100 uM incubated for 30 mins by Hoechst 33342 staining accumulation assay |
CHEMBL5104221 |
| HCT-116 |
EC50 |
> |
100000.0 |
nM |
Cytotoxicity against human HCT-116 cells incubated for 48 hrs by MTT assay |
CHEMBL5104221 |
| Unchecked |
EC50 |
> |
100000.0 |
nM |
Cytotoxicity against paclitaxel-resistant human HCT116tax cells incubated for 48 hrs by MTT assay |
CHEMBL5104221 |
| HCT-116 |
EC50 |
> |
100000.0 |
nM |
Cytotoxicity against human HCT-116 cells overexpressing human MDR1 incubated for 48 hrs by MTT assay |
CHEMBL5104221 |
| HCT-116 |
EC50 |
> |
100000.0 |
nM |
Cytotoxicity against human HCT-116 cells overexpressing human BCRP incubated for 48 hrs by MTT assay |
CHEMBL5104221 |
| HEK293 |
EC50 |
> |
100000.0 |
nM |
Cytotoxicity against human HEK293 cells incubated for 48 hrs by MTT assay |
CHEMBL5104221 |
| HCT-116 |
Activity |
|
|
|
Cytotoxicity against human HCT-116 cells assessed as reduction on cell viability at 100 uM incubated for 48 hrs in presence of paclitaxel by MTT assay |
CHEMBL5104221 |
| HCT-116 |
Activity |
|
|
|
Cytotoxicity against human HCT-116 cells assessed as reduction on cell viability at 100 uM incubated for 48 hrs by MTT assay |
CHEMBL5104221 |
| HCT-116 |
Activity |
|
|
|
Cytotoxicity against human wild type HCT-116 cells assessed as reduction on cell viability at 100 to 200 uM incubated for 48 hrs in presence of paclitaxel by MTT assay |
CHEMBL5104221 |
| Unchecked |
Activity |
|
|
|
Cytotoxicity against paclitaxel-resistant human HCT116tax cells assessed as reduction on cell viability at 100 to 200 uM incubated for 48 hrs in presence of paclitaxel by MTT assay |
CHEMBL5104221 |
| P-glycoprotein 1 |
Inhibition |
|
|
% |
Inhibition of recombinant human P-gp ATPase activity in presence of MgATP preincubated for 40 min measured after 20 min by Pgp-Glo assay |
CHEMBL5104221 |
| HCT-116 |
Activity |
|
|
|
Cytotoxicity against human HCT-116 cells overexpressing human ABCB1 assessed as reduction on ABCB1 gene expression level by RT-qPCR method |
CHEMBL5104221 |
| HCT-116 |
Activity |
|
|
|
Cytotoxicity against human HCT-116 cells overexpressing human ABCG2 assessed as reduction on ABCG2 gene expression level by RT-qPCR method |
CHEMBL5104221 |
