| Adenosine A2 receptor |
Affinity constant |
= |
10.0 |
uM |
Affinity constant for A2 receptor control of adenylate cyclase in adipocytes, heart and brain cells |
CHEMBL1122012 |
| Adenosine receptor |
Affinity constant |
= |
|
|
Inhibition of adenyl cyclase via P site in adipocytes; Inactive |
CHEMBL1122012 |
| Adenosine A1 receptor |
Ki |
= |
150.0 |
nM |
Displacement of [3H]CCPA from adenosine A1 receptor of rat cortical membranes |
CHEMBL1148450 |
| Adenosine A1 receptor |
Ki |
= |
240.0 |
nM |
Displacement of [3H]R-PIA from adenosine A1 receptor of rat cortical membranes |
CHEMBL1148450 |
| Adenosine A1 receptor |
Ki |
= |
210.0 |
nM |
Displacement of [3H]DPCPX from adenosine A1 receptor of rat cortical membranes |
CHEMBL1148450 |
| Adenosine A2a receptor |
Ki |
= |
1130.0 |
nM |
Displacement of [3H]-MSX-2 from Adenosine A2A receptor of rat striatal membranes |
CHEMBL1148450 |
| Adenosine A2a receptor |
Ki |
= |
1180.0 |
nM |
Displacement of [3H]NECA from Adenosine A2A receptor of rat striatal membranes |
CHEMBL1148450 |
| Adenosine A2b receptor |
Ki |
= |
13900.0 |
nM |
Displacement of [3H]PSB-298 from human adenosine A2B receptor expressed in HEK293 cells at 10 uM; Less than 10% inhibition |
CHEMBL1148450 |
| Adenosine A2b receptor |
Ki |
= |
8200.0 |
nM |
Binding affinity towards human adenosine A2B receptor in VA13 fibroblasts as inhibition of adenylate cyclase at 10 uM; Less than 10% inhibition |
CHEMBL1148450 |
| Adenosine A3 receptor |
Ki |
= |
680.0 |
nM |
Displacement of [3H]PSB-11 from human adenosine A3 receptor expressed in CHO cells |
CHEMBL1148450 |
| Adenosine A1 receptor |
IC50 |
= |
680.0 |
nM |
Displacement of [3H]DPCPX from adenosine A1 receptor of rat cortical membranes without GTP |
CHEMBL1148450 |
| Adenosine A1 receptor |
IC50 |
= |
15100.0 |
nM |
Displacement of [3H]DPCPX from adenosine A1 receptor of rat cortical membranes with GTP |
CHEMBL1148450 |
| Adenosine A1 receptor |
Ratio |
= |
22.2 |
|
Binding affinity against adenosine A1 receptor without GTP |
CHEMBL1148450 |
| Adenosine A3 receptor |
IC50 |
= |
71000.0 |
nM |
Inhibition of forskolin-stimulated cAMP accumulation in chinese hamster ovary cell membranes expressing human adenosine A3 receptor |
CHEMBL1148450 |
| Adenosine A3 receptor |
Efficacy |
= |
46.0 |
% |
Percent efficacy for inhibition of human adenosine A3 receptor activity relative to NECA |
CHEMBL1148450 |
| Indolethylamine N-methyltransferase |
Ki |
= |
700000.0 |
nM |
Inhibitory constant towards indole N-methyl-transferase |
CHEMBL1122373 |
| L1210 |
IC50 |
= |
600000.0 |
nM |
Compound was evaluated for its ability to inhibit growth by 50% at 48 hr in L1210 murine leukemia cells |
CHEMBL1124473 |
| L5178Y |
IC50 |
= |
60000.0 |
nM |
Compound was evaluated for its ability to inhibit growth by 50% at 48 hr in L5178Y murine leukemia cells |
CHEMBL1124473 |
| L1210 |
Control |
= |
53.0 |
% |
Inhibition of growth of L1210 murine leukemia cell line in percent of control at 600 uM |
CHEMBL1124473 |
| L1210 |
Activity |
= |
3.64 |
nM (10e6*cells)-1 |
Compound was evaluated for effect on polyamine pools in the L1210 murine leukemia cell lines by the inhibition of put at 600 uM |
CHEMBL1124473 |
| L1210 |
Activity |
= |
1.59 |
nM (10e6*cells)-1 |
Compound was evaluated for effect on polyamine pools in the L1210 murine leukemia cell lines by the inhibition of spermidine synthase at 600 uM |
CHEMBL1124473 |
| L1210 |
Activity |
= |
0.2 |
nM (10e6*cells)-1 |
Compound was evaluated for effect on polyamine pools in the L1210 murine leukemia cell lines by the inhibition of spermine synthase at 600 uM |
CHEMBL1124473 |
| L5178Y |
Control |
= |
57.0 |
% |
Inhibition of growth of L5178Y murine leukemia cell line in percent of control at 60 uM |
CHEMBL1124473 |
| L5178Y |
Activity |
= |
1.24 |
nM (10e6*cells)-1 |
Compound was evaluated for effect on polyamine pools in the L5178Y murine leukemia cell lines by the inhibition of put at 60 uM |
CHEMBL1124473 |
| L5178Y |
Activity |
= |
3.03 |
nM (10e6*cells)-1 |
Compound was evaluated for effect on polyamine pools in the L5178Y murine leukemia cell lines by the inhibition of spermidine synthase at 60 uM |
CHEMBL1124473 |
| L5178Y |
Activity |
= |
0.47 |
nM (10e6*cells)-1 |
Compound was evaluated for effect on polyamine pools in the L5178Y murine leukemia cell lines by the inhibition of spermine synthase at 60 uM |
CHEMBL1124473 |
| Catechol O-methyltransferase |
Ki |
> |
5400000.0 |
nM |
Compound was tested for inhibition of Catechol O-methyltransferase using radiochemical assay |
CHEMBL1121736 |
| Fatty acid synthase |
Ki |
= |
1500000.0 |
nM |
Inhibition constant against Escherichia coli cyclopropane fatty acid synthase |
CHEMBL1148231 |
| Spermidine synthase |
Activity |
= |
44.0 |
% |
Compound was tested for its effect on Bovine brain spermine synthase at 0.01 mM |
CHEMBL1121830 |
| Spermidine synthase |
Activity |
= |
12.0 |
% |
Compound was tested for its effect on Bovine brain spermine synthase at 0.1 mM |
CHEMBL1121830 |
| Spermidine synthase |
Activity |
= |
41.0 |
% |
Compound was tested for its effect on rat prostatic spermidine synthase at 0.1 mM |
CHEMBL1121830 |
| Spermidine synthase |
Activity |
= |
9.0 |
% |
Compound was tested for its effect on rat prostatic spermine synthase at 0.1 mM |
CHEMBL1121830 |
| S-methyl-5-thioadenosine phosphorylase |
Km |
= |
1300.0 |
nM |
The inhibitory constant for MTA phosphorylase activity was determined by using a mouse liver enzyme preparation |
CHEMBL1125934 |
| S-methyl-5-thioadenosine phosphorylase |
Control |
= |
100.0 |
% |
The ability to act as substrates for MTA phosphorylase activity was determined by using a mouse liver enzyme preparation |
CHEMBL1125934 |
| L1210 |
IC50 |
= |
850000.0 |
nM |
The concentration required to inhibit cell growth by 50% was measured on L1210 Leukemic cell line of mouse(48h after exposure) |
CHEMBL1125934 |
| L5178Y |
IC50 |
= |
200000.0 |
nM |
The concentration required to inhibit cell growth by 50% was measured on L5178Y Leukemic cell line of mouse(48h after exposure) |
CHEMBL1125934 |
| CCRF-CEM |
IC50 |
= |
150000.0 |
nM |
The concentration required to inhibit cell growth by 50% was measured on human CCRF-CEM cells (96h after exposure) |
CHEMBL1125934 |
| MOLT-4 |
IC50 |
= |
11000.0 |
nM |
The concentration required to inhibit cell growth by 50% was measured on human MOLT-4 cells (96h after exposure) |
CHEMBL1125934 |
| L1210 |
Activity |
= |
1.93 |
|
Effect of compound on putrescine(PUT) polyamine pool in L1210 murine leukemia cells expressed in terms of nmol/10e6 cells |
CHEMBL1125934 |
| L1210 |
Activity |
= |
1.22 |
|
Effect of compound on spermidine(SPD) polyamine pool in L1210 murine leukemia cells expressed in terms of nmol/10e6 cells |
CHEMBL1125934 |
| L1210 |
Activity |
= |
0.19 |
|
Effect of compound on spermine(SPM) polyamine pool in L1210 murine leukemia cells expressed in terms of nmol/10e6 cells |
CHEMBL1125934 |
| L5178Y |
Activity |
= |
1.85 |
|
Effect of compound on putrescine(PUT) polyamine pool in L5178Y murine leukemia cells expressed as nmol/10e6 cells |
CHEMBL1125934 |
| L5178Y |
Activity |
= |
2.79 |
|
Effect of compound on spermidine(SPD) polyamine pool in L5178Y murine leukemia cells expressed in terms of nmol/10e6 cells |
CHEMBL1125934 |
| L5178Y |
Activity |
= |
0.43 |
|
Effect of compound on spermine(SPM) polyamine pool in L5178Y murine leukemia cells expressed in terms of nmol/10e6 cells |
CHEMBL1125934 |
| Adenosylhomocysteinase |
Activity |
= |
101.0 |
% |
Percentage enzyme activity remaining was measured by the inhibition S-adenosyl-L-homocysteine hydrolase from bovine liver at 0.01 uM |
CHEMBL1125934 |
| Adenosylhomocysteinase |
Activity |
= |
94.0 |
% |
Percentage enzyme activity remaining was measured by the inhibition S-adenosyl-L-homocysteine hydrolase from bovine liver at 10 uM |
CHEMBL1125934 |
| Adenosylhomocysteinase |
Activity |
= |
86.0 |
% |
Percentage enzyme activity remaining was measured by the inhibition S-adenosyl-L-homocysteine hydrolase from bovine liver at 0.1 uM |
CHEMBL1125934 |
| Adenosylhomocysteinase |
Activity |
= |
66.0 |
% |
Percentage enzyme activity remaining was measured by the inhibition S-adenosyl-L-homocysteine hydrolase from bovine liver at 100 uM |
CHEMBL1125934 |
| Adenosylhomocysteinase |
Activity |
= |
48.0 |
% |
Percentage enzyme activity remaining was measured by the inhibition S-adenosyl-L-homocysteine hydrolase from bovine liver at 1 uM |
CHEMBL1125934 |
| S-methyl-5-thioadenosine phosphorylase |
Km |
= |
5000.0 |
nM |
Km for human MTAP |
CHEMBL1140320 |
| S-methyl-5-thioadenosine phosphorylase |
K cat |
= |
0.0065 |
1/sec |
Kcat against human methylthioadenosine phosphorylase expressed in Escherichia coli BL21 DE3 cells |
CHEMBL1139590 |
| S-methyl-5-thioadenosine phosphorylase |
Km |
= |
106000.0 |
nM |
Km against human methylthioadenosine phosphorylase expressed in Escherichia coli BL21 DE3 cells |
CHEMBL1139590 |
| S-methyl-5-thioadenosine phosphorylase |
Ratio |
= |
0.0001 |
1/uM*sec |
Ratio of Kcat to Km against human Methylthioadenosine phosphorylase |
CHEMBL1139590 |
| S-methyl-5-thioadenosine phosphorylase |
K cat |
= |
4.6 |
1/sec |
Kcat against human methylthioadenosine phosphorylase expressed in Escherichia coli BL21 DE3 cells |
CHEMBL1139590 |
| S-methyl-5-thioadenosine phosphorylase |
Km |
= |
4600.0 |
nM |
Km against human methylthioadenosine phosphorylase expressed in Escherichia coli BL21 DE3 cells |
CHEMBL1139590 |
| S-methyl-5-thioadenosine phosphorylase |
Ratio |
= |
3.2 |
1/uM*sec |
Ratio of Kcat to Km against human Methylthioadenosine phosphorylase |
CHEMBL1139590 |
| Unchecked |
Activity |
|
|
|
Inhibition of Escherichia coli DNA methyltransferase at 15 uM after 30 mins |
CHEMBL1142331 |
| Unchecked |
Activity |
|
|
|
Inhibition of M.HhaI DNA methyltransferase expressed in ER1727 cells at 15 uM after 30 mins |
CHEMBL1142331 |
| 5-methylthioadenosine/S-adenosylhomocysteine deaminase |
Km |
= |
44000.0 |
nM |
Activity of Thermotoga maritima S-adenosyl-homocysteine deaminase Tm0936 assessed as ammonia production |
CHEMBL1145524 |
| 5-methylthioadenosine/S-adenosylhomocysteine deaminase |
Kcat |
= |
7.2 |
/s |
Activity of Thermotoga maritima S-adenosyl-homocysteine deaminase Tm0936 assessed as ammonia production |
CHEMBL1145524 |
| 5-methylthioadenosine/S-adenosylhomocysteine deaminase |
Kcat/Km |
= |
1.5 |
10^5/M/s |
Ratio of Kcat to Km for Thermotoga maritima S-adenosyl-homocysteine deaminase Tm0936 assessed as ammonia production |
CHEMBL1145524 |
| Spermidine synthase |
IC50 |
= |
159000.0 |
nM |
Inhibition of Plasmodium falciparum spermidine synthase |
CHEMBL1150259 |
| Trypanosoma brucei brucei |
IC50 |
= |
100000.0 |
nM |
Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei LAB 110 EATRO after 48 hrs by Z1 zoulter counter |
CHEMBL1151452 |
| Trypanosoma brucei brucei |
IC50 |
|
|
|
Antitrypanosomal activity against pentamidine and melarsoprol-resistant bloodstream form of Trypanosoma brucei brucei isolate KETRI 243 after 48 hrs by Z1 zoulter counter |
CHEMBL1151452 |
| Trypanosoma brucei brucei |
IC50 |
|
|
|
Antitrypanosomal activity against pentamidine-resistant bloodstream form of Trypanosoma brucei brucei isolate KETRI 269 after 48 hrs by Z1 zoulter counter |
CHEMBL1151452 |
| Trypanosoma brucei brucei |
IC50 |
|
|
|
Antitrypanosomal activity against diamidine and melarsoprol-resistant bloodstream form of Trypanosoma brucei brucei isolate KETRI 243-As10-3 after 48 hrs by Z1 zoulter counter |
CHEMBL1151452 |
| Unchecked |
Activity |
= |
100.0 |
% |
Activity at bloodstream Trypanosoma brucei brucei 5'-deoxy-5'-(methylthio)-adenosine phosphorylase by spectrophotometry in presence of 50 mM PO4- relative to control |
CHEMBL1151452 |
| Unchecked |
Activity |
= |
100.0 |
% |
Activity at bloodstream Trypanosoma brucei brucei 5'-deoxy-5'-(methylthio)-adenosine phosphorylase by spectrophotometry relative to control |
CHEMBL1151452 |
| Unchecked |
Activity |
= |
100.0 |
% |
Activity at mouse liver 5'-deoxy-5'-(methylthio)-adenosine phosphorylase |
CHEMBL1151452 |
| Unchecked |
Inhibition |
|
|
% |
Inhibition of protein kinase in human HuH7 cells assessed as increase in ATP level at 5 uM after 72 hrs by Kinase-Glo assay |
CHEMBL2040791 |
| PRMT5/MEP50 complex |
Kd |
= |
661.0 |
nM |
Inhibition of streptavidin sensor chip immobilized biotinylated human PRMT5/MEP50 assessed as dissociation constant by SPR analysis |
CHEMBL5046262 |
