Percentage of inhibition of the binding/function of various molecules by tegoprazan
Data show the mean of two data points.
| Target Molecule | Tegoprazan10 μM (% Inhibition) | Assay Reference | ||
|---|---|---|---|---|
| Compound | IC50 | |||
| nM | ||||
| Binding inhibition | ||||
| Adenosine | A1 (h) | 25 | DPCPX | 4.0 |
| A2A (h) | 8 | NECA | 19 | |
| A3 (h) | 36 | IB-MECA | 2.1 | |
| Adrenergic | α1 (r, nonselective) | 3 | Prazosin | 0.45 |
| α2A (h) | 8 | Yohimbine | 6.6 | |
| α2B (h) | 11 | Yohimbine | 9.8 | |
| α2C (h) | 10 | Yohimbine | 0.94 | |
| β1 (h) | 0 | Atenolol | 170 | |
| β2 (h) | 6 | ICI 118551 | 2.6 | |
| β3 (h) | −6 | Cyanopindolol | 140 | |
| Angiotensin | AT1 (h) | −1 | Saralasin | 0.64 |
| Benzodiazepine | BZD (r, central) | 12 | Diazepam | 10 |
| Cannabinoid | CB1 (h) | 3 | CP 55940 | 1.3 |
| CB2 (h) | 23 | WIN 55212-2 | 2.1 | |
| Channels | Ca2+ (r, L, DHP site) | 19 | Nirendipine | 1.7 |
| Ca2+ (r, L, diltiazem site) | −5 | Diltiazem | 26 | |
| Ca2+ (r, L, verapamil site) | −5 | D 600 | 50 | |
| Ca2+ (r, N) | 21 | ω-conotoxin GVIA | 0.0015 | |
| Na+ (r, site 2) | 31 | Veratridine | 4500 | |
| SK+ Ca (r) | −9 | Apamiin | 0.009 | |
| Cl− (r) | −2 | Picrotoxinin | 270 | |
| Cytokine | CXCR4 (h) | 3 | SDF-1α | 0.04 |
| TNF-α (h) | −15 | TNF-α | 0.06 | |
| Cholecystokinin | CCKA (h) | 4 | CCK-8 | 0.27 |
| CCKB (h) | 0 | CCK-8 | 0.27 | |
| Dopamine | D1 (h) | 6 | SCH 23390 | 0.75 |
| D2S (h) | 2 | (+)butaclamol | 5.2 | |
| D2S (h, agonist site) | −11 | 7-OH-DPAT | 2.7 | |
| D3 (h) | 2 | (+)butaclamol | 6.4 | |
| D4.4 (h) | 3 | Clozapine | 56 | |
| Endothelin | ETA (h) | −6 | Endothelin-1 | 0.099 |
| ETB (h) | 9 | Endothelin-3 | 0.061 | |
| GABA | GABAA (r) | −10 | Muscimol | 8.4 |
| GABAB (h) | −7 | CGP 54626 | 12 | |
| Glutamate | AMPA (r) | 1 | L-glutamate | 1300 |
| Kainate (r) | 3 | Kainic acid | 40 | |
| NMDA (r) | 1 | CGS 19755 | 390 | |
| Glycine (r, strychnine insensitive) | −4 | Glycine | 290 | |
| Hormone | GR (h) | 18 | Dexamethasone | 5.3 |
| TH (r) | −6 | T3 | 0.20 | |
| Ghrelin (h, GHS) | 8 | Ghrelin | 0.25 | |
| Motilin (h) | 6 | Motilin | 1.1 | |
| Androgen (h) | −9 | Methyltrienolone | 2.5 | |
| MCH1 (h) | 7 | MCH | 0.19 | |
| Histamine | H1 (h) | −8 | Pyrilamine | 4.8 |
| H2 (h) | 20 | Cimetidine | 270 | |
| H3 (h) | 4 | Rα -Me-histamine | 1.6 | |
| H4 (h) | −5 | Imetit | 4.2 | |
| Imidazoline | I1 (r) | −3 | Rilmenidine | 130 |
| Leukotriene | LTB4 (h, BLT1) | −1 | LTB4 | 0.23 |
| LTD4, (h, CysLT1) | −2 | LTD4 | 1.3 | |
| Melanocoltin | MC1 (r) | 21 | NDP-α-MSH | 0.24 |
| MC3 (h) | 1 | NDP-α-MSH | 0.45 | |
| MC4 (h) | 3 | NDP-α-MSH | 0.53 | |
| Melatonin | ML1 (r) | 13 | Melatonin | 0.16 |
| ML2 (r) | 81 | Melatonin | 40 | |
| MAO | MAO-A (r) | −3 | Clorgyline | 2.0 |
| Muscarinic | M1 (h) | 0 | Pirenzepine | 6.3 |
| M2 (h) | 9 | Methoctramiine | 25 | |
| M3 (h) | −13 | 4-DAMP | 0.28 | |
| M4 (h) | 4 | 4-DAMP | 0.63 | |
| M5 (h) | 2 | 4-DAMP | 0.37 | |
| Neurokinin | NK1 (h) | −10 | [Sar9,Met (O2)11]-SP | 0.36 |
| NK2 (h) | −3 | [Nle10]-NKA(4-10) | 13 | |
| Neuropeptide Y | Y1 (h) | 5 | NPY | 0.23 |
| Nicotine | N (r, neuronal, α4β2) | 1 | Nicotine | 8.5 |
| N (h, muscle-type) | 5 | α-bungarotoxin | 4.9 | |
| Opioid | δ (r, non-selective) | 5 | Haloperidol | 74 |
| δ2 (h, DOP) | 15 | DPDPE | 1.9 | |
| κ (r, KOP) | 23 | U 50488 | 0.61 | |
| μ (h, MOP, agonist site) | −5 | DAMGO | 0.78 | |
| Phencyclidine | PCP (r) | 2 | MK801 | 3.4 |
| PDE | Rolipram (r) | 17 | Rolipram | 1.6 |
| Serotonin | 5-HT1A (h) | 7 | 8-OH-DPTA | 0.63 |
| 5-HT1B (r) | 10 | Serotonin | 13 | |
| 5-HT1D (h) | 6 | Serotonin | 2.4 | |
| 5-HT2A (h) | 33 | Ketanserin | 2.2 | |
| 5-HT2A (h, agonist site) | 1 | (±)DOI | 1.3 | |
| 5-HT2B (h, agonist site) | 46 | (±)DOI | 2.9 | |
| 5-HT2C (h) | −1 | RS-102221 | 5.5 | |
| 5-HT2C (h, agonist site) | −2 | (±)DOI | 2.2 | |
| 5-HT3 (h) | 7 | MDL 72222 | 8.2 | |
| 5-HT4e (h) | 36 | Serotonin | 480 | |
| 5-HT6 (h) | 14 | Serotonin | 230 | |
| 5-HT7 (h) | −6 | Serotonin | 0.56 | |
| Somatostatin | sst4 (h) | 16 | Somatostatin | 7.3 |
| Transporters | NE (h) | 3 | Protriptyline | 12 |
| DA (h) | 4 | BTCP | 11 | |
| GABA (h) | −30 | nipecotic aid | 3200 | |
| Choline (h, CHT1) | 20 | hemicholinium-3 | 6.3 | |
| 5-HT (h) | −4 | Imipramine | 4.0 | |
| Urotensin | UT1 (h) | −4 | urotensin-II | 0.95 |
| Vasopressin | V1a (h) | 0 | [d(CH2)51,Tyr(Me)2]-AVP | 0.97 |
| V2 (h) | 0 | AVP | 1.3 | |
| VIP | VIP1 (h, VPAC1) | 0 | VIP | 0.25 |
| Functional inhibition | ||||
| Enzymes | COX-1 (h) | −19 | Diclofenac | 20 |
| COX-2 (h) | 11 | NS398 | 72 | |
| PDE2 (h) | 26 | EHNA | 4000 | |
| PDE3 (h) | −13 | Milrinone | 160 | |
| PDE4 (h) | 35 | Rolipram | 580 | |
| PDE5 (h) | 9 | Dipyridamole | 1800 | |
| PDE6 (h) | 38 | Zaprinast | 190 | |
| PDE11 (h) | 14 | Dipyridamole | 490 | |
| ACE (h) | −29 | Captopril | 3.6 | |
| Caspase-3 (h) | −1 | Ac-DEVD-CHO | 0.48 | |
| MMP-9 (h) | 1 | GM6001 | 0.61 | |
| Carbonic anhydrase II (h) | −12 | Acetazolamide | 7.8 | |
| Acetylcholinesterase (h) | 3 | Neostigmine | 41 | |
| ATPase (d, Na+/K+)a | 4 | Ouabain | 490 | |
| Kinase | FLT-1 (h, VEGFRK1) | 8 | Staurosporine | 7.9 |
| p38α (h) | 18 | SB202190 | 31 | |
| Abl (h) | 3 | Staurosporine | 120 | |
| CaMK2α (h) | 4 | AIP | 430 | |
| Lyn (h) | 18 | Staurosporine | 48 | |
| ZAP70 (h) | −9 | Staurosporine | 34 | |
d, dog; h, human origin; MAO, monoamine oxidase; PDE, phosphodiesterase; r, rat origin; VIP, vasoactive intestinal peptide.
↵a tegoprazan 30 μM.