Histamine H1 human. 2. 10. 1. Histamine H2 human. 2. 10. -10. Histamine H3 human. 2. 10. 4. Histamine H4 human. 2. 10. 8. Imidazoline I2, Central rat. 2. 10. 3.
Table S1 Binding properties of T1-11 toward 208 proteins. Target Species Adenosine A1 human Adenosine A2A human Adenosine A2B human Adenosine A3 human Adrenergic α1, Non-Selective rat Adrenergic α1A rat Adrenergic α1B rat Adrenergic α1D human Adrenergic α2, Non-Selective rat Adrenergic α2A human Adrenergic α2B human Adrenergic α2C human Adrenergic β, Non-Selective rat Adrenergic β1 human Adrenergic β3 human Adrenomedullin AM1 human Adrenomedullin AM2 human Aldosterone rat Anaphylatoxin C5a human Androgen (Testosterone) human Angiotensin AT1 human Angiotensin AT2 human APJ human Atrial Natriuretic Factor (ANF) guinea pig Benzodiazepine, Peripheral rat Bombesin BB1 human Bombesin BB2 human Bombesin BB3 human Bombesin, Non-Selective rat Bradykinin B1 human Bradykinin B2 human Calcitonin human Calcitonin Gene-Related, Peptide CGRP1 human Calcium Channel L-Type, Benzothiazepine rat Calcium Channel L-Type, Dihydropyridine rat Calcium Channel L-Type, Phenylalkylamin. rat Calcium Channel N-Type rat Cannabinoid CB1 human Cannabinoid CB2 human Chemokine CCR1 human Chemokine CCR2B human Chemokine CCR4 human Chemokine CCR5 human Chemokine CX3CR1 human Chemokine CXCR1/2 (IL-8, Non-Selective) human Chemokine CXCR2 (IL-8RB) human Cholecystokinin CCK. (CCK8) human Cholecystokinin CCK. (CCKA) human Colchicine rat Corticotropin Releasing Factor, CRF1 human Cyclooxygenase COX-2 human
n value 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2
Concentration (μM) % Inhibition 10 23 10 58 10 0 10 103 10 -3 10 -14 10 3 10 8 10 2 10 -8 10 2 10 10 10 10 10 7 10 -1 10 11 10 9 10 2 10 2 10 3 10 -5 10 3 10 21 10 5 10 3 10 -5 10 3 10 12 10 6 10 -8 10 -9 10 15 10 6 10 -8 10 -4 10 -7 10 1 10 -7 10 -2 10 -3 10 0 10 5 10 -8 10 -1 10 10 10 0 10 -5 10 -3 10 -2 10 1 10 0
Dopamine D1 Dopamine D2L Dopamine D2S Dopamine D3 Dopamine D4.2 Dopamine D4.4 Dopamine D4.7 Dopamine D5 Endothelin ETA Endothelin ETB Epidermal Growth Factor (EGF) Erythropoietin EPOR Estrogen ERα Estrogen ERβ G Protein-Coupled Receptor, GPR103 G Protein-Coupled Receptor, GPR8 GABAA, Agonist Site GABAA, Benzodiazepine, Central, Flunitrazepam GABAA, Benzodiazepine, Central, Ro-15-1788 GABAA, Chloride Channel, TBOB GABAA, Chloride Channel, TBPS GABAA, Non-Selective GABAB1A GABAB1B Gabapentin Galanin GAL1 Galanin GAL2 Glucocorticoid Glutamate, AMPA Glutamate, Kainate Glutamate, NMDA, Agonism Glutamate, NMDA, Glycine Glutamate, NMDA, Phencyclidine Glutamate, NMDA, Polyamine Glutamate, Non-Selective Glycine, Strychnine-Sensitive Growth Hormone, Secretagogue (GHS, Ghrelin) Histamine H1 Histamine H2 Histamine H3 Histamine H4 Imidazoline I2, Central Imidazoline I2, Peripheral Inositol Trisphosphate IP3 Insulin Interleukin IL-1 Interleukin IL-2 Interleukin IL-6 Leptin Leukotriene, BLT (LTB4) Leukotriene, Cysteinyl CysLT1 Leukotriene, Cysteinyl CysLT2
human human human human human human human human human human human human human human human human rat rat rat rat rat rat human human rat human human human rat rat rat rat rat rat rat rat human human human human human rat rat rat rat mouse mouse human mouse human human human
2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2
10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10
-13 13 10 -7 3 8 3 2 3 2 -5 3 32 40 2 15 4 6 1 -3 6 5 -1 -5 8 0 0 -10 -9 11 10 7 -2 10 -1 10 -4 1 -10 4 8 3 10 3 4 4 0 -3 6 -6 -4 10
Lipoxygenase 12-LO Lipoxygenase 15-LO Lipoxygenase 5-LO Melanocortin MC1 Melanocortin MC3 Melanocortin MC4 Melanocortin MC5 Melatonin MT, Non-Selective Melatonin MT1 Melatonin MT2 Motilin Muscarinic M1 Muscarinic M2 Muscarinic M3 Muscarinic M4 Muscarinic M5 Muscarinic, Non-Selective, Central Muscarinic, Oxotremorine-M Neuromedin U NMU1 Neuromedin U NMU2 Neuropeptide Y Y1 Neuropeptide Y Y2 Neurotensin NT1 Neurotensin, Non-Selective N-Formyl Peptide Receptor, FPR1 N-Formyl Peptide Receptor-like, FPRL1 Nicotinic Acetylcholine Nicotinic Acetylcholine α1, Bungarotoxin Nicotinic Acetylcholine α7, Bungarotoxin Opiate δ (OP1, DOP) Opiate κ (OP2, KOP) Opiate μ (OP3, MOP) Opiate, Non-Selective Orexin OX1 Orexin OX2 Orphanin ORL1 Phorbol Ester Phosphodiesterase PDE1 Phosphodiesterase PDE1 Phosphodiesterase PDE10A1 Phosphodiesterase PDE3 Phosphodiesterase PDE4 Phosphodiesterase PDE5 Phosphodiesterase PDE6 Platelet Activating Factor (PAF) Platelet-Derived Growth Factor (PDGF) Potassium Channel [KA] Potassium Channel [KATP] Potassium Channel [SKCA] Potassium Channel HERG Progesterone Progesterone PR-B Prostanoid CRTH2
human rabbit human human human human human chicken human human human human human human human human rat rat human human human human human mouse human human human human rat human human human rat human human human mouse bovine human human human human human human human mouse rat hamster rat human bovine human human
2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2
10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10
9 14 25 3 3 5 1 -3 -4 -20 -2 -1 4 -6 9 0 12 -7 -1 5 6 4 11 15 5 5 6 3 -1 19 6 5 -13 -13 -7 10 9 26 17 1 0 0 4 21 7 -4 1 6 1 -2 9 -8 0
Prostanoid DP Prostanoid EP2 Prostanoid EP4 Prostanoid, Thromboxane A2 (TP) Purinergic P2X Purinergic P2Y Rolipram Ryanodine RyR3 Serotonin (5-Hydroxytryptamine) 5-HT1, Non-Selective Serotonin (5-Hydroxytryptamine) 5-HT1A Serotonin (5-Hydroxytryptamine) 5-HT1B Serotonin (5-Hydroxytryptamine) 5-HT2, Non-Selective Serotonin (5-Hydroxytryptamine) 5-HT2A Serotonin (5-Hydroxytryptamine) 5-HT2B Serotonin (5-Hydroxytryptamine) 5-HT2C Serotonin (5-Hydroxytryptamine) 5-HT3 Serotonin (5-Hydroxytryptamine) 5-HT4 Serotonin (5-Hydroxytryptamine) 5-HT5A Serotonin (5-Hydroxytryptamine) 5-HT6 Serotonin (5-Hydroxytryptamine) 5-HT7 Sigma σ1 Sigma σ2 Sigma, Non-Selective Sodium Channel, Site 2 Somatostatin sst1 Somatostatin sst2 Somatostatin sst3 Somatostatin sst4 Somatostatin sst5 Tachykinin NK1 Tachykinin NK2 Tachykinin NK3 Thyroid Hormone Thyrotropin Releasing Hormone (TRH) Transforming Growth Factor-β (TGF-β) Transporter, Adenosine Transporter, Choline Transporter, Dopamine Transporter, GABA Transporter, Glycin.e Transporter, Monoamine Transporter, Norepinephrine (NET) Transporter, Serotonin (5-Hydroxytryptamine) (SERT) Tumor Necrosis Factor (TNF), Non-Selective Urotensin II Vanilloid Vascular Endothelial Growth Factor (VEGF) Vasoactive Intestinal Peptide VIP1 Vasopressin V1A Vasopressin V1B Vasopressin V2 Vitamin D3
human human human human rabbit rat rat rat rat human rat rat human human human human guinea pig human human human human rat guinea pig rat human human human human human human human human rat rat mouse guinea pig rat human rat rat rabbit human human human human rat human human human human human human
2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2
10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10 10
17 10 -6 1 11 17 -6 -1 10 9 3 15 19 5 27 5 1 -7 12 2 7 -3 -3 3 -3 9 15 5 4 3 3 -3 -9 -4 -1 84 -10 -6 8 1 -6 6 5 -2 6 8 16 2 0 -18 -5 6
