 |
|
| Nouveaux tests |
|
|
| in vitro pharmacology |
|
| non-peptide receptors |
 Adenosine |
|
|
A1 |
G127 |
|
|
A2A (agonist effect) |
2527 |
|
|
A2B (antagonist radioligand) |
0005 |
|
|
A3 |
G107 |
|
|
| Adrenergic |
|
|
alpha 2A |
G120 |
|
|
alpha 2C |
G006 |
|
|
| Cannabinoid |
|
|
CB1 |
G012 |
|
|
CB2 |
G013 |
|
|
| Dopamine |
|
|
D1 (antagonist radioligand) |
0044 |
|
|
D2S (antagonist radioligand) |
0046 |
|
|
D2S |
G116 |
|
|
D3 (agonist radioligand) |
1660 |
|
|
D3 |
G016 |
|
|
D4.4 |
G017 |
|
|
| Free fatty acid |
|
|
FFA3 (GPR41) |
G143 |
|
|
| GABA |
|
|
GABAA1 (alpha1,beta2,gamma2) (agonist radioligand) |
3051 |
|
|
GABAB |
G111 |
|
|
GABAA - agonist conventional patch-clamp |
2859 |
|
|
| Glutamate |
|
|
AMPA (agonist radioligand) |
0064 |
|
|
| Histamine |
|
|
H2 (antagonist radioligand) |
0079 |
|
|
H3 |
G021 |
|
|
H4 |
G125 |
|
|
| Melatonin |
|
|
MT1 (ML1A) |
G136 |
|
|
MT2 (ML1B) |
G028 |
|
|
MT3 (ML2) (agonist radioligand) |
0088 |
|
|
| Muscarinic |
|
|
M (non-selective) (antagonist radioligand) |
0089 |
|
|
M2 |
G030 |
|
|
M4 |
G032 |
|
|
| Prostanoid |
|
|
EP1 |
G035 |
|
|
EP3 (agonist radioligand) |
2774 |
|
|
EP3 |
G122 |
|
|
EP4 (agonist radioligand) |
0441 |
|
|
EP4 |
G037 |
|
|
| Serotonin |
|
|
5-HT1A |
G044 |
|
|
5-HT1B |
G126 |
|
|
5-HT1D |
G112 |
|
|
5-HT2A |
G181 |
|
|
5-HT2B |
G183 |
|
|
5-HT2C |
G184 |
|
|
5-HT6 (agonist radioligand) |
0142 |
|
|
5-HT7 (agonist radioligand) |
0144 |
|
|
5-HT7 |
G051 |
|
|
|
| peptide receptors |
| Apelin |
|
|
APJ (apelin) (agonist radioligand) |
2154 |
|
|
APJ (apelin) |
G146 |
|
|
| Calcitonin gene-related peptide |
|
|
CGRP |
G058 |
|
|
| Chemokines |
|
|
CCR2 (agonist radioligand) |
0362 |
|
|
CCR2 |
G138 |
|
|
CXCR2 (IL-8B) |
G113 |
|
|
CXCR4 |
G114 |
|
|
| Complement 5a |
|
|
C5a |
G064 |
|
|
| N-formyl peptide |
|
|
fMLP |
G069 |
|
|
| Galanin |
|
|
galanin (non-selective) (agonist radioligand) |
0061 |
|
|
| Glucagon |
|
|
GLP-1 (agonist radioligand) |
0228 |
|
|
glucagon (agonist radioligand) |
1407 |
|
|
| Growth factors |
|
|
PDGF (agonist radioligand) |
0070 |
|
|
| Melanocortin |
|
|
MC2 |
G080 |
|
|
| Neuropeptide Y |
|
|
Y1 |
G088 |
|
|
Y2 (agonist radioligand) |
0107 |
|
|
| Opioid and opioid-like |
|
|
delta 2 (DOP) |
G129 |
|
|
kappa (KOP) |
G090 |
|
|
mu (MOP) |
G091 |
|
|
NOP (ORL1) |
G119 |
|
|
| Somatostatin |
|
|
sst1 (agonist radioligand) |
1940 |
|
|
sst1 |
G095 |
|
|
sst4 |
G096 |
|
|
sst5 |
G097 |
|
|
| Thyrotropin releasing hormone |
|
|
TRH1 (agonist radioligand) |
1616 |
|
|
| Vasoactive intestinal peptide |
|
|
VPAC2 (VIP2) (agonist radioligand) |
0487 |
|
|
|
| nuclear receptors |
| Non-steroid nuclear receptors |
|
|
PPARalpha |
G131 |
|
|
PPARgamma (agonist radioligand) |
0641 |
|
|
TR (TH) (agonist radioligand) |
0156 |
|
|
|
| ion channels |
| Membrane ligand-gated channels |
|
|
AMPA (agonist radioligand) |
0064 |
|
|
GABAA1 (alpha1,beta2,gamma2) (agonist radioligand) |
3051 |
|
|
GABAA - agonist automated patch-clamp, |
3260 |
|
|
GABAA - antagonist automated patch-clamp |
3393 |
|
|
GABAA - potentiation automated patch-clamp |
3394 |
|
|
GABAA - agonist conventional patch-clamp |
2859 |
|
|
GABAA - antagonist conventional patch-clamp |
3395 |
|
|
GABAA - potentation conventional patch-clamp |
3396 |
|
|
| Voltage-gated channels |
|
|
L (verapamil site) (phenylalkylamine) (antagonist radioligand) |
0163 |
|
|
N (antagonist radioligand) |
0164 |
|
|
KV (antagonist radioligand) |
0166 |
|
|
|
| amine transporters |
| Adenosine |
|
|
adenosine uptake |
3374 |
|
|
|
| Kinases |
| Protein-tyrosine kinases |
|
|
c-kit kinase |
3070 |
|
|
CTK |
2638 |
|
|
FAK |
3065 |
|
|
Fyn kinase |
0212 |
|
|
EphA4 kinase |
1702 |
|
|
EphA5 kinase |
2640 |
|
|
FGFR2 kinase |
2893 |
|
|
FLT-1 kinase (VEGFR1) |
3068 |
|
|
HER4/ErbB4 kinase |
1875 |
|
|
KDR kinase (VEGFR2) |
2864 |
|
|
Ron kinase |
3067 |
|
|
| Protein-serine/threonine kinases |
|
|
ASK1 |
2124 |
|
|
CK1epsilon |
2630 |
|
|
GCK (MAP4K2) |
2590 |
|
|
Akt3/PKBgamma |
2925 |
|
|
DLK1 (MAP3K12) |
2620 |
|
|
CDK4 (cycD1) |
2876 |
|
|
GRK2 (ADRBK1) |
2200 |
|
|
CDK6 (cycD3) |
2909 |
|
|
MRCKalpha |
2629 |
|
|
MEKK4 (MAP3K4) |
2759 |
|
|
MSK2 |
1983 |
|
|
CDK8 (cycC) |
2911 |
|
|
RAF-1/MEK1 kinase |
1703 |
|
|
MKK6 /p38alpha (mutant active) |
1679 |
|
|
CK2 (casein kinase 2) |
2913 |
|
|
MST2 kinase |
2761 |
|
|
MARK1 |
3362 |
|
|
MARK3 |
2789 |
|
|
DYRK2 |
2788 |
|
|
MARK4 |
1967 |
|
|
PAK1 |
1934 |
|
|
PAK2 |
2932 |
|
|
PKCeta |
2046 |
|
|
PKCiota |
2121 |
|
|
PKCbeta 2 |
2750 |
|
|
PKG1beta |
1730 |
|
|
HIPK2 |
2915 |
|
|
Pim1 kinase |
2919 |
|
|
PRKX |
2681 |
|
|
PKD1 (PKCµ) |
2204 |
|
|
JNK1 |
2880 |
|
|
JNK2 |
3368 |
|
|
PKD3 |
1982 |
|
|
ROCK1 |
3364 |
|
|
SIK |
2921 |
|
|
JNK3 |
2916 |
|
|
p38beta2 kinase (SAPK2b2) |
1960 |
|
|
RSK3 |
2682 |
|
|
p38delta kinase |
3116 |
|
|
PCTAIRE1 kinase |
2025 |
|
|
| Other kinases |
|
|
AurC/Aur3 kinase |
1842 |
|
|
CDC7 /ASK |
2764 |
|
|
NEK1 |
1931 |
|
|
NEK2 |
2939 |
|
|
NEK7 |
2588 |
|
|
PEK (EIF2AK3) |
2589 |
|
|
PLK1 |
2049 |
|
|
TBK1 |
3347 |
|
|
TTK |
2767 |
|
|
ULK1 |
3346 |
|
|
ULK2 |
3348 |
|
|
| Atypical kinases |
|
|
mTOR kinase (FRAP1) |
2941 |
|
|
|
| Non-kinase enzymes |
| Miscellaneous enzymes |
|
|
HDAC1 |
2491 |
|
|
| Proteases |
|
|
MT1-MMP (MMP-14) |
0670 |
|
|
|
| ADME-Tox |
|
| in vitro drug absorption / drug transport |
| A-B Permeability |
|
|
A-B Permeability (Caco-2, pH 6.5/7.4) |
3318 |
|
|
A-B Permeability (Caco-2, pH 7.4/7.4) |
3319 |
|
|
| B-A Permeability |
|
|
B-A Permeability (Caco-2, pH 6.5/7.4) |
3320 |
|
|
B-A Permeability (Caco-2, pH 7.4/7.4) |
3321 |
|
|
| P-glycoprotein Interactions |
|
|
P-gp Inhibition (Caco-2, 3H-digoxin substrate) |
3349 |
|
|
|
|
| Nouveaux profils 2010 |
|
|
| In Vitro Pharmacology |
| PDE High Throughput Profile |
|
