Inhibition of B-Raf activated MEK2 (unknown origin) assessed as ERK2-mediated MBP phosphorylation after 30 mins by ELISA
|
Homo sapiens
|
1.6
nM
|
|
Inhibition of B-Raf activated MEK1 (unknown origin) assessed as ERK2-mediated MBP phosphorylation after 30 mins by ELISA
|
Homo sapiens
|
3.4
nM
|
|
Growth inhibition of human MDA-MB-175-VII cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
96.0
nM
|
|
Growth inhibition of human RKO cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
18.0
nM
|
|
Growth inhibition of human HCT8 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
55.0
nM
|
|
Growth inhibition of human NCI-H508 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
23.0
nM
|
|
Growth inhibition of human DLD1 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
632.0
nM
|
|
Growth inhibition of human T84 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
61.0
nM
|
|
Growth inhibition of human KM12 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
23.0
nM
|
|
Growth inhibition of human SW837 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
74.0
nM
|
|
Growth inhibition of human LS1034 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
5.0
nM
|
|
Growth inhibition of human COLO205 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
1.0
nM
|
|
Growth inhibition of human SW1463 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
4.0
nM
|
|
Growth inhibition of human HT-29 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
2.0
nM
|
|
Growth inhibition of human SW480 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
37.0
nM
|
|
Growth inhibition of human SW1417 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
3.0
nM
|
|
Growth inhibition of human COR-L23 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
329.0
nM
|
|
Growth inhibition of human A549 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
34.0
nM
|
|
Growth inhibition of human NCI-H1355 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
52.0
nM
|
|
Growth inhibition of human NCI-H1792 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
53.0
nM
|
|
Growth inhibition of human NCI-H23 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
29.0
nM
|
|
Growth inhibition of human Calu6 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
4.0
nM
|
|
Growth inhibition of human MV522 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
2.0
nM
|
|
Growth inhibition of human SW900 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
127.0
nM
|
|
Growth inhibition of human A427 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
22.0
nM
|
|
Growth inhibition of human Calu3 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
158.0
nM
|
|
Growth inhibition of human NCI-H727 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
2.0
nM
|
|
Growth inhibition of human MDA-MB-175-VII cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
16.0
nM
|
|
Growth inhibition of human EFM19 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
30.0
nM
|
|
Growth inhibition of human RKO cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
5.0
nM
|
|
Growth inhibition of human HCT8 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
14.0
nM
|
|
Growth inhibition of human NCI-H508 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
8.0
nM
|
|
Growth inhibition of human DLD1 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
93.0
nM
|
|
Growth inhibition of human T84 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
30.0
nM
|
|
Growth inhibition of human KM12 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
10.0
nM
|
|
Growth inhibition of human SW837 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
25.0
nM
|
|
Growth inhibition of human LS1034 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
4.0
nM
|
|
Growth inhibition of human COLO205 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
1.0
nM
|
|
Growth inhibition of human SW1463 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
4.0
nM
|
|
Growth inhibition of human HT-29 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
1.0
nM
|
|
Growth inhibition of human SW480 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
26.0
nM
|
|
Growth inhibition of human SW1417 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
3.0
nM
|
|
Growth inhibition of human COR-L23 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
37.0
nM
|
|
Growth inhibition of human A549 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
16.0
nM
|
|
Growth inhibition of human NCI-H1355 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
27.0
nM
|
|
Growth inhibition of human NCI-H1792 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
35.0
nM
|
|
Growth inhibition of human NCI-H23 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
20.0
nM
|
|
Growth inhibition of human Calu6 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
3.0
nM
|
|
Growth inhibition of human MV522 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
1.0
nM
|
|
Growth inhibition of human NCI-H1155 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
10.0
nM
|
|
Growth inhibition of human SW1573 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
38.0
nM
|
|
Growth inhibition of human HOP62 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
50.0
nM
|
|
Growth inhibition of human SW900 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
72.0
nM
|
|
Growth inhibition of human A427 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
10.0
nM
|
|
Growth inhibition of human HCC827 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
40.0
nM
|
|
Growth inhibition of human Calu3 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
39.0
nM
|
|
Growth inhibition of human NCI-H727 cells at 1:10 molar ratio of compound in presence of N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecar- boxamide incubated for 72 hrs by Cell-titer-Glo reagent based assay
|
Homo sapiens
|
2.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
62.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
9.0
nM
|
|
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
|
Homo sapiens
|
76.63
%
|
|
Antiproliferative activity against human A375 cells assessed as reduction in cell viability
|
Homo sapiens
|
0.74
nM
|
|
Inhibition of ERK1/2 phosphorylation at Thr202/Tyr204 residues in human MIAPaCa2 cells grown under 3D anchorage-independent soft-agar conditions at 50 nM incubated for 2 to 8 hrs by Western blotting analysis relative to control
|
Homo sapiens
|
65.0
%
|
|
Inhibition of ABCB1 in human A2780/ADR cells assessed as potentiation of daunorubicin-induced cytotoxicity measured after 72 hrs by MTT assay
|
Homo sapiens
|
247.0
nM
|
|
Inhibition of MEK1 (unknown origin)
|
Homo sapiens
|
0.7
nM
|
|
Inhibition of MEK2 (unknown origin)
|
Homo sapiens
|
14.9
nM
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
19.64
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
8.399
%
|
|
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
|
Chlorocebus sabaeus
|
-0.19
%
|
|
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
|
Chlorocebus sabaeus
|
-0.36
%
|
|
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
|
Chlorocebus sabaeus
|
-0.36
%
|
|
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
|
Chlorocebus sabaeus
|
-0.19
%
|
|
Antiproliferative activity against human A375 cells harboring BRAF V600E mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
|
Homo sapiens
|
2.4
nM
|
|
Antiproliferative activity against human MDA-MB-231 cells harboring KRAS G13D/BRAF G464V mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
|
Homo sapiens
|
18.0
nM
|
|
Antiproliferative activity against human HCT116 cells harboring KRAS G13D mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
|
Homo sapiens
|
19.0
nM
|
|
Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
|
Homo sapiens
|
460.0
nM
|
|
Antiproliferative activity against human HL60 cells harboring NRAS K61L mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
|
Homo sapiens
|
3.0
nM
|
|
Antiproliferative activity against human KYSE-520 cells
|
Homo sapiens
|
10.0
nM
|
|
Inhibition of MEK in human KYSE-520 cells assessed as reduction in p-ERK levels
|
Homo sapiens
|
1.0
nM
|
|