BAF3 |
Function assay |
0.01 to 10 uM |
1 hr |
Inhibition of TEL-fused wild type Ret (unknown origin) phosphorylation at Y1062/Y905 expressed in mouse BAF3 cells at 0.01 to 10 uM after 1 hr by Western blot analysis |
26652860 |
BAF3 |
Function assay |
0.01 to 10 uM |
1 hr |
Inhibition of TEL-fused Ret S891A mutant (unknown origin) phosphorylation at Y1062/Y905 expressed in mouse BAF3 cells at 0.01 to 10 uM after 1 hr by Western blot analysis |
26652860 |
BAF3 |
Function assay |
0.01 to 10 uM |
1 hr |
Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BAF3 cells assessed as suppression of phosphorylation of PLCgamma at Y783 at 0.01 to 10 uM after 1 hr by Western blot analysis |
26652860 |
BAF3 |
Function assay |
0.01 to 10 uM |
1 hr |
Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BAF3 cells assessed as suppression of phosphorylation of Shc at Y317 at 0.01 to 10 uM after 1 hr by Western blot analysis |
26652860 |
TT |
Function assay |
1 to 10 uM |
4 hrs |
Inhibition of RET C634W mutant in human TT cells assessed as suppression of PLCgamma phosphorylation at Y783 at 1 to 10 uM after 4 hrs by Western blot analysis |
26652860 |
TT |
Function assay |
1 to 10 uM |
4 hrs |
Inhibition of RET C634W mutant in human TT cells assessed as suppression of ERK phosphorylation at T202/Y204 at 1 to 10 uM after 4 hrs by Western blot analysis |
26652860 |
TT |
Function assay |
1 to 10 uM |
4 hrs |
Inhibition of RET C634W mutant in human TT cells assessed as suppression of AKT phosphorylation at T308/S473 at 1 to 10 uM after 4 hrs by Western blot analysis |
26652860 |
TT |
Function assay |
1 uM |
4 hrs |
Inhibition of autophosphorylation of RET C634W mutant at Y1062 in human TT cells at 1 uM after 4 hrs by Western blot analysis |
26652860 |
TT |
Apoptosis assay |
1 uM |
96 hrs |
Induction of apoptosis in human TT cells expressing Ret C634W mutant at 1 uM after 96 hrs by annexinV/PI staining-based flow cytometric analysis |
26652860 |
A549 |
Cytotoxicity assay |
10 uM |
72 hrs |
Cytotoxicity against human A549 cells at 10 uM after 72 hrs by Incucyte live-cell imaging analysis |
29407963 |
E98NT? |
Growth Inhibition Assay |
0.01-10 μM |
|
IC50=89 nM |
23484006 |
TT |
Function assay |
1 uM |
|
Inhibition of Ret-driven oncogenic transformation of human TT cells at 1 uM by soft agar assay |
26652860 |
BaF3 |
Growth inhibition assay |
|
48 hrs |
Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.01 μM. |
26652860 |
BA/F3 |
Growth inhibition assay |
|
48 hrs |
Inhibition of wild type TEL-fused RET (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.05 μM. |
26652860 |
TT |
Growth inhibition assay |
|
10 days |
Inhibition of RET C634W mutant in human TT cells assessed as cell growth inhibition after 10 days by MTT assay, GI50 = 0.12 μM. |
26652860 |
BA/F3 |
Growth inhibition assay |
|
48 hrs |
Inhibition of TEL-fused Ret V804M mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.89 μM. |
26652860 |
BaF3 |
Growth inhibition assay |
|
48 hrs |
Inhibition of TEL-fused Ret V804L mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.91 μM. |
26652860 |
Nthy-ori 3-1 |
Cytotoxicity assay |
|
10 days |
Cytotoxicity against human Nthy-ori 3-1 cells after 10 days by MTT assay, GI50 = 4.93 μM. |
26652860 |
TT |
Function assay |
|
4 hrs |
Inhibition of autophosphorylation of RET C634W mutant at Y905 in human TT cells at 1 uM after 4 hrs by Western blot analysis |
26652860 |
PC3 |
Function assay |
|
1 to 3 hrs |
Inhibition of c-Met phosphorylation in human PC3 cells incubated for 1 to 3 hrs, IC50 = 1.9 μM. |
26717201 |
MDA-MB-231 |
Function assay |
|
1 to 3 hrs |
Inhibition of AXL phosphorylation in human MDA-MB-231 cells incubated for 1 to 3 hrs, IC50 = 5 μM. |
26717201 |
BAF3 |
Function assay |
|
1 to 3 hrs |
Inhibition of FLT3 (unknown origin) phosphorylation transfected in mouse BAF3 cells incubated for 1 to 3 hrs, IC50 = 7.5 μM. |
26717201 |
MDA-MB-231 |
Function assay |
|
1 to 3 hrs |
Inhibition of KIT (unknown origin) phosphorylation transfected in human MDA-MB-231 cells incubated for 1 to 3 hrs, IC50 = 42 μM. |
26717201 |
BA/F3 |
Function assay |
|
48 hrs |
Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay, IC50 = 0.014 μM. |
26874741 |
Sf21 |
Function assay |
|
15 mins |
Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay, IC50 = 0.016 μM. |
26874741 |
BA/F3 |
Function assay |
|
48 hrs |
Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay, IC50 = 0.19 μM. |
26874741 |
BA/F3 |
Function assay |
|
48 hrs |
Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay, IC50 = 0.19 μM. |
26874741 |
BA/F3 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay, IC50 = 0.0219 μM. |
27068889 |
Sf21 |
Function assay |
|
60 mins |
Inhibition of wild type N-terminal GST-tagged recombinant human RET (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA, IC50 = 0.003 μM. |
27131066 |
Sf21 |
Function assay |
|
60 mins |
Inhibition of N-terminal GST-tagged recombinant human RET V804M mutant (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA, IC50 = 0.811 μM. |
27131066 |
BaF3 |
Function assay |
|
72 hrs |
Inhibition of CCDC6-RET (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by SRB/CCK-8 assay, IC50 = 0.889 μM. |
27131066 |
BaF3 |
Function assay |
|
72 hrs |
Inhibition of CCDC6-RET (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by SRB/CCK-8 assay, IC50 = 0.889 μM. |
27131066 |
HepG2 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 0.012 μM. |
28412159 |
EBC1 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay, IC50 = 0.0514 μM. |
28412159 |
H1299 |
Growth inhibition assay |
|
72 hrs |
Growth inhibition of human H1299 cells incubated for 72 hrs by CCK8 assay, IC50 = 1.919 μM. |
28651979 |
MCF7 |
Growth inhibition assay |
|
72 hrs |
Growth inhibition of human MCF7 cells incubated for 72 hrs by CCK8 assay, IC50 = 2.889 μM. |
28651979 |
A549 |
Growth inhibition assay |
|
72 hrs |
Growth inhibition of human A549 cells incubated for 72 hrs by CCK8 assay, IC50 = 4.205 μM. |
28651979 |
T47D |
Growth inhibition assay |
|
72 hrs |
Growth inhibition of human T47D cells incubated for 72 hrs by CCK8 assay, IC50 = 4.448 μM. |
28651979 |
H460 |
Growth inhibition assay |
|
72 hrs |
Growth inhibition of human H460 cells incubated for 72 hrs by CCK8 assay, IC50 = 5.669 μM. |
28651979 |
HuH7 |
Antiproliferative assay |
|
48 hrs |
Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay, IC50 = 4.348 μM. |
29057042 |
A498 |
Antiproliferative assay |
|
48 hrs |
Antiproliferative activity against human A498 cells after 48 hrs by MTT assay, IC50 = 8.456 μM. |
29057042 |
NCI-H727 |
Antiproliferative assay |
|
48 hrs |
Antiproliferative activity against human NCI-H727 cells after 48 hrs by MTT assay, IC50 = 14.01 μM. |
29057042 |
BAF3 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against mouse BAF3 cells harboring TRP-MET after 72 hrs by CCK-8 assay, IC50 = 0.024 μM. |
29146452 |
EBC1 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay, IC50 = 0.0048 μM. |
30248654 |
MKN45 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.0069 μM. |
30248654 |
SNU5 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay, IC50 = 0.0121 μM. |
30248654 |
BAF3 |
Function assay |
|
72 hrs |
Inhibition of TPR-tagged met (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.01986 μM. |
30248654 |
NCI-H460 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 0.0401 μM. |
30248654 |
MGHU3 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human MGHU3 cells after 72 hrs by CellTiter-Glo assay |
30309671 |
RT112 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human RT112 cells after 72 hrs by CellTiter-Glo assay |
30309671 |
MDA-MB-231 |
Growth Inhibition Assay |
|
|
IC50= 6421 nM |
21926191 |
SNU-16 |
Growth Inhibition Assay |
|
|
IC50=1149 nM |
21926191 |
SNU-1? |
Growth Inhibition Assay |
|
|
IC50=5223 nM |
21926191 |
Hs746T? |
Growth Inhibition Assay |
|
|
IC50=9.9 nM |
21926191 |
SNU-5? |
Growth Inhibition Assay |
|
|
IC50= 19 nM |
21926191 |
U87MG |
Growth Inhibition Assay |
|
|
IC50=1851 nM |
21926191 |
H441? |
Growth Inhibition Assay |
|
|
IC50=21700 nM |
21926191 |
H69 |
Growth Inhibition Assay |
|
|
IC50=20200 nM |
21926191 |
PC3 |
Growth Inhibition Assay |
|
|
IC50=10800 nM |
21926191 |
MTC-TT |
Growth Inhibition Assay |
|
|
IC50=0.04 + 0.03 μM |
21470995 |
MZ-CRC |
Growth Inhibition Assay |
|
|
IC50> 5 μM |
21470995 |
TPC-1 |
Growth Inhibition Assay |
|
|
IC50=0.06 + 0.02 μM |
21470995 |
NIH-3T3/TPR-Met |
Function assay |
|
|
Inhibition of cell proliferation in mouse NIH-3T3/TPR-Met cells, IC50 = 1 μM. |
24996144 |
BA/F3 |
Growth inhibition assay |
|
|
Inhibition of TEL-fused VEGFR2 (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition, GI50 = 0.003 μM. |
26652860 |
Ba/F3 |
Function assay |
|
|
Inhibition of RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 0.07 μM. |
27814560 |
TT |
Function assay |
|
|
Inhibition of RET C634W mutant in human TT cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 0.26 μM. |
27814560 |
Ba/F3 |
Function assay |
|
|
Inhibition of RET V804M mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 0.74 μM. |
27814560 |
Nthy-ori 3-1 |
Cytotoxicity assay |
|
|
Cytotoxicity against human Nthy-ori 3-1 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 2.92 μM. |
27814560 |
A673 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells |
29435139 |
DAOY |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells |
29435139 |
Saos-2 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells |
29435139 |
BT-37 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells |
29435139 |
RD |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells |
29435139 |
SK-N-SH |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells |
29435139 |
BT-12 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells |
29435139 |
NB1643 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells |
29435139 |
OHS-50 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells |
29435139 |
Rh41 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells |
29435139 |
A673 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) |
29435139 |
U-2 OS |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells |
29435139 |
OHS-50 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells |
29435139 |
Rh41 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells |
29435139 |
SJ-GBM2 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells |
29435139 |
SK-N-MC |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells |
29435139 |
NB-EBc1 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells |
29435139 |
LAN-5 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells |
29435139 |
Rh18 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells |
29435139 |
SJ-GBM2 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells |
29435139 |
TC32 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells |
29435139 |
Saos-2 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells |
29435139 |