| Homo sapiens |
Cytochrome P450 1A2 |
AC50 |
nan |
None |
None |
| Homo sapiens |
Cytochrome P450 2C19 |
AC50 |
nan |
None |
None |
| Homo sapiens |
Cytochrome P450 2C9 |
AC50 |
nan |
None |
None |
| Homo sapiens |
Cytochrome P450 2D6 |
AC50 |
nan |
None |
None |
| Homo sapiens |
Cytochrome P450 3A4 |
AC50 |
nan |
None |
None |
| Homo sapiens |
Equilibrative nucleoside transporter 4 |
Activity |
-11.7 |
nanoampere |
10.1124/dmd.111.042432 |
| Homo sapiens |
Equilibrative nucleoside transporter 4 |
Activity |
-0.627 |
nanoampere |
10.1124/dmd.111.042432 |
| Homo sapiens |
HEK293 |
Potency |
1457.5 |
nM |
None |
| Homo sapiens |
Multidrug and toxin extrusion protein 1 |
Activity |
nan |
None |
10.1038/nrd3028 |
| Homo sapiens |
Multidrug and toxin extrusion protein 2 |
Activity |
nan |
None |
10.1038/nrd3028 |
| Homo sapiens |
Nuclear factor NF-kappa-B p105 subunit |
Potency |
11220.2 |
nM |
None |
| Homo sapiens |
P-glycoprotein 1 |
Activity |
nan |
None |
10.1016/s0928-0987(00)00097-x |
| Homo sapiens |
P-glycoprotein 1 |
Activity |
nan |
None |
None |
| Homo sapiens |
Potassium channel subfamily K member 9 |
Inhibition |
6.1 |
% |
10.1021/acs.jmedchem.9b00248 |
| Homo sapiens |
Solute carrier family 22 member 1 |
Activity |
168.0 |
uM |
10.1124/mol.63.3.489 |
| Homo sapiens |
Solute carrier family 22 member 1 |
Activity |
nan |
None |
10.1038/nrd3028 |
| Homo sapiens |
Solute carrier family 22 member 1 |
Activity |
nan |
None |
10.1089/dna.1997.16.871 |
| Homo sapiens |
Solute carrier family 22 member 1 |
Inhibition |
nan |
% |
10.1124/dmd.110.037960 |
| Homo sapiens |
Solute carrier family 22 member 1 |
Ki |
158000.0 |
nM |
None |
| Homo sapiens |
Solute carrier family 22 member 1 |
Ki |
161000.0 |
nM |
None |
| Homo sapiens |
Solute carrier family 22 member 1 |
Ki |
163000.0 |
nM |
10.1124/mol.51.6.913 |
| Homo sapiens |
Solute carrier family 22 member 1 |
Km |
2320.0 |
nM |
10.1021/jm8003152 |
| Homo sapiens |
Solute carrier family 22 member 1 |
Km |
229000.0 |
nM |
None |
| Homo sapiens |
Solute carrier family 22 member 1 |
Vmax |
696.0 |
RFU/min |
10.1021/jm8003152 |
| Homo sapiens |
Solute carrier family 22 member 11 |
Activity |
nan |
None |
10.1074/jbc.275.6.4507 |
| Homo sapiens |
Solute carrier family 22 member 2 |
Activity |
nan |
None |
10.1038/nrd3028 |
| Homo sapiens |
Solute carrier family 22 member 2 |
Activity |
nan |
None |
10.1074/jbc.m108472200 |
| Homo sapiens |
Solute carrier family 22 member 2 |
IC50 |
156000.0 |
nM |
10.1023/a:1019870831174 |
| Homo sapiens |
Solute carrier family 22 member 2 |
Km |
31000.0 |
nM |
10.1089/dna.1997.16.871 |
| Homo sapiens |
Solute carrier family 22 member 2 |
Km |
63000.0 |
nM |
10.1097/01.asn.0000019413.78751.46 |
| Homo sapiens |
Solute carrier family 22 member 2 |
Km |
76000.0 |
nM |
10.1089/dna.1997.16.871 |
| Homo sapiens |
Solute carrier family 22 member 2 |
Km |
431000.0 |
nM |
10.1097/01.asn.0000019413.78751.46 |
| Homo sapiens |
Solute carrier family 22 member 3 |
Activity |
nan |
None |
10.1152/ajprenal.2000.279.3.f449 |
| Homo sapiens |
Solute carrier family 22 member 3 |
IC50 |
10300000.0 |
nM |
10.1007/s002100000335 |
| Homo sapiens |
Solute carrier family 22 member 3 |
Ki |
1372000.0 |
nM |
10.1152/ajprenal.2000.279.3.f449 |
| Homo sapiens |
Solute carrier family 22 member 4 |
Km |
436000.0 |
nM |
None |
| Homo sapiens |
Solute carrier family 22 member 5 |
Activity |
40.0 |
% |
None |
| Homo sapiens |
Solute carrier family 22 member 5 |
Activity |
53.6 |
% |
None |
| Homo sapiens |
Solute carrier family 22 member 5 |
Activity |
nan |
None |
None |
| Homo sapiens |
Solute carrier family 22 member 6 |
Activity |
nan |
None |
10.1124/mol.56.3.570 |
| Homo sapiens |
Solute carrier family 22 member 8 |
Activity |
nan |
None |
10.1006/bbrc.1998.9978 |
| Homo sapiens |
Solute carrier family 22 member 8 |
Activity |
nan |
None |
10.1124/mol.59.5.1277 |
| Homo sapiens |
Solute carrier organic anion transporter family member 1B1 |
Inhibition |
25.9 |
% |
10.1021/jm300212s |
| Homo sapiens |
Solute carrier organic anion transporter family member 1B3 |
Inhibition |
4.9 |
% |
10.1021/jm300212s |
| Homo sapiens |
Solute carrier organic anion transporter family member 2B1 |
Inhibition |
6.7 |
% |
10.1021/jm300212s |
| Homo sapiens |
T-cell line |
IC50 |
1000.0 |
nM |
10.1016/S0960-894X(97)00163-7 |
| Homo sapiens |
Thyroid stimulating hormone receptor |
Potency |
3981.1 |
nM |
None |
| Homo sapiens |
Voltage-gated potassium channel subunit Kv1.1 |
IC50 |
30000.0 |
nM |
10.1021/acs.jmedchem.6b01262 |
| Mus musculus |
Choline transporter |
Ki |
260015.96 |
nM |
10.1016/j.bmcl.2010.06.090 |
| Mus musculus |
Mus musculus |
AUC |
2410.0 |
ng.hr.mL-1 |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
AUC |
2840.0 |
ng.hr.mL-1 |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
AUC |
9100.0 |
ng.hr.mL-1 |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
AUC |
9840.0 |
ng.hr.mL-1 |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
C0 |
22.7 |
ug ml-1 |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
C0 |
67.4 |
ug ml-1 |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
CL |
0.08 |
ml/min |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
CL |
0.09 |
ml/min |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
CL |
0.12 |
ml/min |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
CL |
0.19 |
ml/min |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
CL |
16.9 |
mL.min-1.kg-1 |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
CL |
58.7 |
mL.min-1.kg-1 |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
Drug recovery |
62.0 |
% |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
Drug recovery |
95.0 |
% |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
T1/2 |
0.2 |
hr |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
T1/2 |
0.31 |
hr |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
Vdss |
0.318 |
L.kg-1 |
10.1124/dmd.112.044875 |
| Mus musculus |
Mus musculus |
Vdss |
1.52 |
L.kg-1 |
10.1124/dmd.112.044875 |
| Mus musculus |
Solute carrier family 22 member 1 |
Activity |
nan |
None |
10.1128/mcb.21.16.5471-5477.2001 |
| Mus musculus |
Solute carrier family 22 member 1 |
IC50 |
540.0 |
nM |
10.1016/s0006-291x(02)00926-9 |
| Mus musculus |
Solute carrier family 22 member 1 |
Ki |
128000.0 |
nM |
None |
| Mus musculus |
Solute carrier family 22 member 1 |
Km |
38000.0 |
nM |
10.1002/hep.510290530 |
| Mus musculus |
Solute carrier family 22 member 2 |
IC50 |
3500.0 |
nM |
10.1016/s0006-291x(02)00926-9 |
| Mus musculus |
Solute carrier family 22 member 2 |
Km |
35700.0 |
nM |
10.1016/s0006-291x(02)00926-9 |
| Mus musculus |
Solute carrier family 22 member 3 |
Activity |
nan |
None |
10.1152/ajprenal.2000.279.3.f449 |
| Mus musculus |
Solute carrier family 22 member 3 |
Km |
1900000.0 |
nM |
10.1152/ajprenal.2000.279.3.f449 |
| Mus musculus |
Solute carrier family 22 member 4 |
Km |
452000.0 |
nM |
10.1074/jbc.m005340200 |
| Mus musculus |
Solute carrier family 22 member 5 |
Activity |
15.4 |
% |
10.1124/mol.59.2.358 |
| Mus musculus |
Solute carrier family 22 member 5 |
Km |
216000.0 |
nM |
10.1074/jbc.m005340200 |
| Rattus norvegicus |
Brain |
Compound recovery |
nan |
None |
10.1124/dmd.110.035998 |
| Rattus norvegicus |
Brain |
Fu |
1.0 |
None |
10.1124/dmd.110.035998 |
| Rattus norvegicus |
Brain |
Kp |
8.95 |
None |
10.1124/dmd.110.035998 |
| Rattus norvegicus |
Brain |
Vd |
9.0 |
L.kg-1 |
10.1124/dmd.110.035998 |
| Rattus norvegicus |
Muscarinic acetylcholine receptor M1 |
Potency |
3162.3 |
nM |
None |
| Rattus norvegicus |
Solute carrier family 22 member 1 |
Activity |
nan |
None |
10.1038/sj.bjp.0702065 |
| Rattus norvegicus |
Solute carrier family 22 member 1 |
Ki |
46600.0 |
nM |
None |
| Rattus norvegicus |
Solute carrier family 22 member 1 |
Ki |
100000.0 |
nM |
None |
| Rattus norvegicus |
Solute carrier family 22 member 1 |
Ki |
286000.0 |
nM |
10.1016/s0006-2952(00)00334-8 |
| Rattus norvegicus |
Solute carrier family 22 member 1 |
Km |
35000.0 |
nM |
10.1074/jbc.271.51.32599 |
| Rattus norvegicus |
Solute carrier family 22 member 1 |
Km |
38000.0 |
nM |
None |
| Rattus norvegicus |
Solute carrier family 22 member 1 |
Km |
42000.0 |
nM |
10.1074/jbc.272.26.16548 |
| Rattus norvegicus |
Solute carrier family 22 member 1 |
Km |
95000.0 |
nM |
10.1038/372549a0 |
| Rattus norvegicus |
Solute carrier family 22 member 1 |
Km |
129000.0 |
nM |
10.1124/mol.56.6.1254 |
| Rattus norvegicus |
Solute carrier family 22 member 1 |
Km |
251000.0 |
nM |
10.1016/s0006-2952(00)00334-8 |
| Rattus norvegicus |
Solute carrier family 22 member 2 |
Activity |
nan |
None |
10.1124/mol.56.1.1 |
| Rattus norvegicus |
Solute carrier family 22 member 2 |
Ki |
52200.0 |
nM |
None |
| Rattus norvegicus |
Solute carrier family 22 member 2 |
Km |
33800.0 |
nM |
10.1016/s0005-2736(99)00005-x |
| Rattus norvegicus |
Solute carrier family 22 member 2 |
Km |
45000.0 |
nM |
None |
| Rattus norvegicus |
Solute carrier family 22 member 2 |
Km |
48000.0 |
nM |
10.1152/ajprenal.1999.277.6.f890 |
| Rattus norvegicus |
Solute carrier family 22 member 2 |
Km |
91000.0 |
nM |
10.1152/ajprenal.2001.281.3.f454 |
| Rattus norvegicus |
Solute carrier family 22 member 2 |
Km |
141000.0 |
nM |
10.1093/toxsci/47.2.181 |
| Rattus norvegicus |
Solute carrier family 22 member 2 |
Km |
160000.0 |
nM |
10.1074/jbc.m004645200 |
| Rattus norvegicus |
Solute carrier family 22 member 2 |
Km |
393000.0 |
nM |
10.1152/ajprenal.1999.277.6.f890 |
| Rattus norvegicus |
Solute carrier family 22 member 3 |
Activity |
41.0 |
% |
10.1074/jbc.273.26.15971 |
| Rattus norvegicus |
Solute carrier family 22 member 3 |
Km |
2500000.0 |
nM |
10.1074/jbc.273.26.15971 |
| Rattus norvegicus |
Solute carrier family 22 member 3 |
Km |
6200000.0 |
nM |
10.1074/jbc.273.26.15971 |
| Rattus norvegicus |
Solute carrier family 22 member 4 |
Activity |
nan |
None |
10.1016/s0005-2736(00)00189-9 |
| Rattus norvegicus |
Solute carrier family 22 member 4 |
IC50 |
1000000.0 |
nM |
10.1016/s0005-2736(00)00189-9 |
| Rattus norvegicus |
Solute carrier family 22 member 5 |
Activity |
4.0 |
% |
None |
| Rattus norvegicus |
Solute carrier family 22 member 5 |
Km |
63000.0 |
nM |
None |
| Rattus norvegicus |
Solute carrier family 22 member 6 |
Activity |
nan |
None |
10.1074/jbc.272.30.18526 |
| Rattus norvegicus |
Solute carrier family 22 member 6 |
Activity |
nan |
None |
10.1074/jbc.272.48.30088 |
| Rattus norvegicus |
Solute carrier family 22 member 7 |
Activity |
nan |
None |
10.1016/s0014-5793(98)00585-7 |
| Rattus norvegicus |
Solute carrier family 22 member 8 |
Activity |
nan |
None |
10.1074/jbc.274.19.13675 |
| Rattus norvegicus |
Solute carrier organic anion transporter family member 1A1 |
Activity |
nan |
None |
10.1007/s004240100697 |
| Rattus norvegicus |
Solute carrier organic anion transporter family member 1A4 |
Activity |
nan |
None |
10.1007/s004240100697 |
| Rattus norvegicus |
Solute carrier organic anion transporter family member 1A5 |
Activity |
nan |
None |
10.1007/s004240100697 |
| Rattus norvegicus |
Solute carrier organic anion transporter family member 1B2 |
Activity |
nan |
None |
10.1007/s004240100697 |
| Rattus norvegicus |
Thioredoxin reductase 1, cytoplasmic |
Potency |
37685.8 |
nM |
None |
| Trypanosoma brucei |
6-phospho-1-fructokinase |
Potency |
33807.8 |
nM |
None |
| None |
ADMET |
Drug excretion |
30.0 |
% |
10.1124/dmd.112.044875 |
| None |
ADMET |
Drug excretion |
35.0 |
% |
10.1124/dmd.112.044875 |
| None |
Unchecked |
IC50 |
7900000.0 |
nM |
10.1016/j.bmcl.2004.05.031 |
| None |
Unchecked |
Potency |
29081.0 |
nM |
None |