Table 1.
Compounds repurchased for concentration-response testing
| Compound type | Cat. No. | Product Name | Target | Pathway | Concentration-response profile |
|---|---|---|---|---|---|
| I | HY-10204 | OSI-930 | Apoptosis; c-Fms; c-Kit; VEGFR | Apoptosis; Protein Tyrosine Kinase/RTK | T |
| I | HY-10295 | SB 202190 | Apoptosis; Autophagy; p38 MAPK | Apoptosis; Autophagy; MAPK/ERK Pathway | 2 |
| I | HY-10342 | Enzastaurin | Apoptosis; Autophagy; PKC | Apoptosis; Autophagy; Epigenetics; TGF-beta/Smad | 1 |
| I | HY-10435A | SKF-82958 (hydrobromide) | Dopamine Receptor | GPCR/G Protein; Neuronal Signaling | 2 |
| I | HY-10472 | LY2811376 | Beta-secretase | Neuronal Signaling | 1 |
| I | HY-107854 | N-Acetyl-5-hydroxytryptamine | Endogenous Metabolite; Trk Receptor | Metabolic Enzyme/Protease; Neuronal Signaling; Protein Tyrosine Kinase/RTK | 2 |
| I | HY-11010 | AS601245 | JNK | MAPK/ERK Pathway | 1 |
| I | HY-112149 | ZL0420 | Epigenetic Reader Domain | Epigenetics | 2 |
| I | HY-112613 | UCB9608 | PI4K | PI3K/Akt/mTOR | 1 |
| I | HY-112667 | CU-CPT-9a | Toll-like Receptor (TLR) | Immunology/Inflammation | 2 |
| I | HY-114269 | (−)-(S)-B-973B | nAChR | Membrane Transporter/Ion Channel; Neuronal Signaling | 1 |
| E | HY-116790A | (+)-Penbutolol | Adrenergic Receptor | GPCR/G Protein; Neuronal Signaling | T |
| I | HY-117626 | LP-935509 | Others | Others | 2 |
| I | HY-12013 | PD153035 (Hydrochloride) | EGFR | JAK/STAT Signaling; Protein Tyrosine Kinase/RTK | T |
| I | HY-120934 | C25-140 | E1/E2/E3 Enzyme; TNF Receptor | Apoptosis; Metabolic Enzyme/Protease | 2 |
| E | HY-121186 | Bevantolol (hydrochloride) | Adrenergic Receptor; Calcium Channel | GPCR/G Protein; Membrane Transporter/Ion Channel; Neuronal Signaling | 2 |
| I | HY-122856 | AZ12601011 | TGF-β Receptor | TGF-beta/Smad | 2 |
| I | HY-123999 | CD38 inhibitor 1 | Others | Others | 1 |
| I | HY-12409 | PFI-3 | Epigenetic Reader Domain | Epigenetics | 2 |
| I | HY-12528 | DBPR108 | Dipeptidyl Peptidase | Metabolic Enzyme/Protease | 1 |
| E | HY-125837A | MS31 (trihydrochloride) | Epigenetic Reader Domain | Epigenetics | T |
| I | HY-126290 | Ropsacitinib | JAK | Epigenetics; JAK/STAT Signaling; Stem Cell/Wnt | 2 |
| I | HY-12787 | L-779450 | Autophagy; Raf | Autophagy; MAPK/ERK Pathway | 2 |
| I | HY-12949 | ML204 | TRP Channel | Membrane Transporter/Ion Channel; Neuronal Signaling | 2 |
| I | HY-13288 | Org 27,569 | Cannabinoid Receptor | GPCR/G Protein; Neuronal Signaling | 2 |
| I | HY-13519 | TRAM-34 | Potassium Channel | Membrane Transporter/Ion Channel | 2 |
| I | HY-14581 | Palomid 529 | Apoptosis; mTOR | Apoptosis; PI3K/Akt/mTOR | 1 |
| I | HY-15124 | (S)-(−)-Bay-K-8644 | Calcium Channel | Membrane Transporter/Ion Channel; Neuronal Signaling | 1 |
| E | HY-15227 | EPZ004777 | Apoptosis; Histone Methyltransferase | Apoptosis; Epigenetics | T |
| I | HY-15427 | GDC-0834 | Btk | Protein Tyrosine Kinase/RTK | 2 |
| I | HY-15427B | GDC-0834 (S-enantiomer) | Btk | Protein Tyrosine Kinase/RTK | 2 |
| I | HY-15438 | SB 415286 | Apoptosis; GSK-3 | Apoptosis; PI3K/Akt/mTOR; Stem Cell/Wnt | 2 |
| I | HY-15456 | NVP-BVU972 | c-Met/HGFR | Protein Tyrosine Kinase/RTK | 2 |
| I | HY-15681 | Senexin A | CDK | Cell Cycle/DNA Damage | 2 |
| I | HY-16425 | RG2833 | HDAC | Cell Cycle/DNA Damage; Epigenetics | 2 |
| I | HY-18700 | BRD73954 | HDAC | Cell Cycle/DNA Damage; Epigenetics | 2 |
| I | HY-18938 | Selonsertib | Apoptosis; MAP3K | Apoptosis; MAPK/ERK Pathway | 1 |
| I | HY-18976 | UF010 | HDAC | Cell Cycle/DNA Damage; Epigenetics | 1 |
| I | HY-19562 | PF-06260933 | MAP4K | MAPK/ERK Pathway | 1 |
| E | HY-19756 | OTX008 | Galectin | Immunology/Inflammation | 2 |
| I | HY-19834 | Fenebrutinib | Btk | Protein Tyrosine Kinase/RTK | 1 |
| I | HY-19836 | Zimlovisertib | IRAK | Immunology/Inflammation | T |
| I | HY-50858 | Ruxolitinib (phosphate) | Autophagy; JAK; Mitophagy | Autophagy; Epigenetics; JAK/STAT Signaling; Stem Cell/Wnt | T |
| I | HY-50865 | PDE-9 inhibitor | Phosphodiesterase (PDE) | Metabolic Enzyme/Protease | IA |
| I | HY-59090 | 1-Azakenpaullone | GSK-3 | PI3K/Akt/mTOR; Stem Cell/Wnt | 1 |
| I | HY-70050C | Alosetron (Hydrochloride) | 5-HT Receptor | GPCR/G Protein; Neuronal Signaling | 1 |
| I | HY-76772 | Cevimeline (hydrochloride hemihydrate) | mAChR | GPCR/G Protein; Neuronal Signaling | 2 |
| I | HY-79511 | FAAH-IN-2 | Autophagy; FAAH | Autophagy; Metabolic Enzyme/Protease; Neuronal Signaling | 1 |
| I | HY-100482 | CPI-637 | Epigenetic Reader Domain; Histone Acetyltransferase | Epigenetics | 2 |
| I | HY-100726 | GNE-272 | Epigenetic Reader Domain; Histone Acetyltransferase | Epigenetics | 1 |
| I | HY-100740C | (1α,1′S,4β)-Lanabecestat | Beta-secretase | Neuronal Signaling | 2 |
| I | HY-101027 | GSK 4027 | Epigenetic Reader Domain; Histone Acetyltransferase | Epigenetics | IA |
| I | HY-101474A | Zanubrutinib | Btk | Protein Tyrosine Kinase/RTK | T |
| I | HY-101494 | Temuterkib | ERK | MAPK/ERK Pathway; Stem Cell/Wnt | 2 |
| I | HY-101736 | AMG9810 | TRP Channel | Membrane Transporter/Ion Channel; Neuronal Signaling | T |
| I | HY-101855 | Anle138b | Amyloid-β | Neuronal Signaling | 2 |
| I | HY-B0371 B | (R)-Terazosin | Adrenergic Receptor | GPCR/G Protein; Neuronal Signaling | 1 |
| I | HY-B0371D | (S)-Terazosin | Adrenergic Receptor | GPCR/G Protein; Neuronal Signaling | 2 |
| E | HY-B0381 | Betaxolol | Adrenergic Receptor | GPCR/G Protein; Neuronal Signaling | 2 |
| I | HY-B0553 | Methazolamide | Carbonic Anhydrase | Metabolic Enzyme/Protease | IA |
| I | HY-B0588 | Brinzolamide | Carbonic Anhydrase | Metabolic Enzyme/Protease | 1 |
| E | HY-B0949 | Protriptyline (hydrochloride) | AChE | Neuronal Signaling | T |
| E | HY-B1213 | Trimipramine (maleate) | 5-HT Receptor; Bacterial | Anti-infection; GPCR/G Protein; Neuronal Signaling | T |
Compounds are identified as inhibitors (I) or enhancers (E) of neuronal tau pathology. The resulting concentration-response curve profile obtained for each compound is indicated, with 1 = discernible upper and lower asymptotes; 2 = concentration-dependent inhibition without clear upper and/or lower asymptotes; T = toxic; IA = inactive.