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Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.

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Probe Reports from the NIH Molecular Libraries Program [Internet].

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Figure 4MDS Pharma Lead Profiling Screen of 68 GPCRs, ion channels and transporters against CID 25067404 (ML077) (SID-56405641) at a concentration of 10 μM.

TargSpecies% Inhibition (10 μM) CID 25067404
Adenosine A1human31
Adenosine A2human38
Adenosine A3human38
Adrenergic α1Arat33
Adrenergic α1Brat3
Adrenergic α1Dhuman16
Adrenergic α2Ahuman−7
Adrenergic β1human10
Adrenergic β2human9
Androgen (testosterone)ARrat4
Bradykinin B1human6
Bradykinin B2human2
Calcium channel L-type, benzothiazepinerat10
Calcium channel L-type, dihydropyridinerat−2
Calcium channel N-typerat−4
Dopamine D1human8
Dopamine D2Shuman−3
Dopamine D3human−1
Dopamine D4.2human−12
Endothelin ETAhuman0
Endothelin ETBhuman−3
Epidermal Growth Factor (EGF)human−1
Estrogen ER αhuman10
G protein-coupled receptor GPR103human12
GABAA Flunitrazepam, centralrat25
GABAA Muscimol, centralrat1
GABAB1Ahuman1
Glucocorticoidhuman7
Glutamate, Kainaterat11
Glutamate, NMDA, Agonismrat33
Glutamate, NMDA, Glycinerat6
Glutamate, NMDA, Phencyclidinerat2
Histamine H1human7
Histamine H2human7
Histamine H3human7
Imidazoline I2, Centralrat6
Interleukin IL-1mouse6
Leukotriene, Cysteinyl CysLT1human10
Melatonin MT1human7
Muscarinic M1human2
Muscarinic M2human−9
Muscarinic M3human5
Neuropeptide Y Y1human3
Neuropeptide Y Y2human9
Nicotinic Acetylcholinehuman3
Nicotinic Acetylcholine 1 α, Bungarotoxinhuman1
Opiateδ (OP1, DOP)human20
Opiate κ (OP2, KOP)human−11
Opiate μ (OP3, MOP)human−3
Phorbol Estermouse24
Platelet Activating Factor (PAF)human4
Potassium Channel [KATP]hamster10
Potassium Channel hERGhuman10
Prostanoid EP4human−4
Purinergic P2Xrabbit−18
Purinergic P2Yrat8
Rolipramrat3
Serotonin (5-Hydroxytryptamine) 5-HT1Ahuman15
Serotonin (5-Hydroxytryptamine) 5-HT3human−7
Sigma σ1human−5
Sigma σ2rat15
Sodium Channel, Site 2rat0
Tachykinin NK1human−10
Thyroid Hormonerat3
Transporter, Dopamine (DAT)human28
Transporter, GABArat0
Transporter, Norepinephrine (NET)human34
Transporter, Serotonin (5-Hydroxytryptamine) (SERT)human2

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