Table 1.
Fifty-seven preliminary positive hits from drug screening with decreased PMR and 4 with increased PMR in 725 compounds NIHCC at 10-µM concentration
| Name | Result | Mechanism | Pubchem ID | Reference | Drug Library Plate |
|---|---|---|---|---|---|
| Topotecan | Decreased migration | Anti-neoplastic topo I inhibitor | 46386667 | (64, 99) | NIHCC Plate_1_A8 |
| SDM25N | Decreased migration | Gamma-receptor antagonist | 46387008 | (75) | NIHCC Plate_1_C5 |
| Vincristine | Decreased migration | Vinca-alkaloid-inhibitor of mitosis | 46386588 | (57, 87) | NIHCC Plate_1_G8 |
| Vindesine | Decreased migration | Vinca-alkaloid-inhibitor of mitosis | 46386586 | (87) | NIHCC Plate_1_H11 |
| Adenosine, N-(2-hydroxycyclopentyl)-, (1S-trans) | Decreased migration | Activation of purine receptors A1 and A2 | 46387015 | (110) | NIHCC Plate_2_A6 |
| Ezetimibe | Decreased migration | inhibits absorption of cholesterol | 46386640 | (2, 37) | NIHCC Plate_2_A8 |
| 8-Azaspiro[4.5]decane-7,9-dione, 8-[2-][(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amino[ethyl]-,monomethanesulfonate | Decreased migration | Anticonvulsant | 46387017 | (84) | NIHCC Plate_2_A10 |
| N,N′-diacetyl-1,6-diaminohexane | Decreased migration | Experimental compound; used in production of nylon | 46386869 | N/A | NIHCC Plate_2_B2 |
| Cefatrizine propylene glycol | Decreased migration | Cephalosporin | 46386659 | (81) | NIHCC Plate_2_B3 |
| Oxymetholone | Decreased migration | Anabolic steroid | 46386778 | (7, 80) | NIHCC Plate_2_B10 |
| Anastrozole | Decreased migration | Nonsteroidal aromatase inhibitor | 46386543 | (79, 97) | NIHCC Plate_2_C7 |
| Rimcazole | Decreased migration | Sigma-receptor antagonist | 46387003 | (42) | NIHCC Plate_2_D4 |
| Zolmitriptan | Decreased migration | Triptan-selective agonist of serotonin 1B and 1D receptor | 46386880 | (74, 89) | NIHCC Plate_2_E11 |
| Artesunate | Decreased migration | Semi-synthetic derivative of artemisinin | 46386645 | (52) | NIHCC Plate_2_H6 |
| Nimetazepam | Decreased migration | Benzodiazepine | 46386768 | (56) | NIHCC Plate_2_H8 |
| Ramipril | Increased migration* | ACE inhibitor | 46386770 | (69) | NIHCC Plate_3_B2 |
| Ampiroxicam | Increased migration* | Prodrug of piroxicam; NSAID-reversible cox-1 inhibitor | 46386688 | (17, 33) | NIHCC Plate_3_E4 |
| Glycine, N-[2-(acetylthio)methyl]-1-oxo-3-phenylpropyl-,phenylmethyl ester | Increased migration* | Amino acid; neurotransmitter in CNS | 46386930 | (8, 20, 65, 117) | NIHCC Plate_3_E6 |
| Triptolide | Decreased migration | Anti-inflammatory; podocyte protective | 46386571 | (12, 16, 46) | NIHCC Plate_3_H2 |
| Ethylestrenol | Decreased migration | Anabolic steroid (Pregnane steroids)-little androgenic effect | 46386573 | (114) | NIHCC Plate_3_H4 |
| Midazolam HCl | Increased migration* | Benzodiazepine-GABA potentiator | 46386603 | (76, 103) | NIHCC Plate_3_H6 |
| Lomerizine DiHCl | Decreased migration | Ca channel blocker | 46386707 | (45, 94) | NIHCC Plate_4_A4 |
| Pancuronium | Decreased migration | Nondepolarizing muscle relaxant; competitive acetylcholine antagonist at NMJ | 46386853 | (29) | NIHCC Plate_4_B3 |
| Trazodone HCl | Decreased migration | Antidepressant; binds 5HT2; selective reuptake inhibitor | 46386915 | (73) | NIHCC Plate_4_B8 |
| Metronidazole | Decreased migration | Nitroimidazole antibiotic; inhibiting bacterial DNA synthesis | 46386860 | (121) | NIHCC Plate_4_B9 |
| Saquinavir mesylate | Decreased migration | HIV protease inhibitor | 46386596 | (28) | NIHCC Plate_4_C6 |
| Tegaserod maleate | Decreased migration | 5HT4 agonist; used for IBS | 46386624 | (15) | NIHCC Plate_4_C7 |
| Diphenylcyclopropenone | Decreased migration | Local irritant | 46386897 | (106) | NIHCC Plate_4_C8 |
| Nifekalant HCl | Decreased migration | Class III anti-arrhythmic; inhibits hERG channel | 46386697 | (36, 50) | NIHCC Plate_4_C11 |
| Bifemelane | Decreased migration | Neuroprotective; mechanism not well understood | 46386922 | (82, 86) | NIHCC Plate_4_D6 |
| Loratidine | Decreased migration | Second generation H1 receptor antagonist | 46386837 | (14) | NIHCC Plate_4_D7 |
| Mesoridazine | Decreased migration | Phenothiazine; adrenergic blockade; hERG cell blockade | 46386921 | (22, 108) | NIHCC Plate_4_D8 |
| Irinotecan HCl | Decreased migration | Antineoplastic-topo I inhibitor | 46386616 | (18) | NIHCC Plate_4_D10 |
| Rifapentine | Decreased migration | Antibiotic; inhibits RNA polymerase in bacteria | 46386637 | (70) | NIHCC Plate_4_D11 |
| Vinorelbine bitatrate | Decreased migration | Vinca-alkaloid-inhibitor of mitosis | 46386815 | (57, 87) | NIHCC Plate_4_E4 |
| Indatraline | Decreased migration | Monoamine transporter inhibitor | 46386808 | (47, 115) | NIHCC Plate_4_E5 |
| Ketorolac | Decreased migration | NSAID; COX1 and COX2 inhibition | 46386614 | (48) | NIHCC Plate_4_E9 |
| Ethynylestradiol | Decreased migration | Synthetic estrogen derivative | 46386858 | (98) | NIHCC Plate_4_F9 |
| Cetraxate HCl | Decreased migration | Anti-ulcer cytoprotective agent (GI tract) | 46386678 | (66) | NIHCC Plate_4_F10 |
| HTMT | Decreased migration | H1/H2 agonist | 46386998 | (91) | NIHCC Plate_4_F11 |
| SR 57,227A | Decreased migration | 5HT3 agonist | 46386849 | (11) | NIHCC Plate_4_G9 |
| Tripelennamine HCl | Decreased migration | H1 antagonist | 46386917 | (119) | NIHCC Plate_4_H9 |
| 5-Methoxytryptamine | Decreased migration | Tryptamine derivative (melatonin)-agonist of 5HT1,2,4,6,7 receptors) | 46387021 | (34) | NIHCC Plate_4_H11 |
| Nifedipine | Decreased migration | Ca-channel blocker | 46386790 | (21, 77, 107a) | NIHCC Plate_5_F8 |
| Doxapram | Decreased migration | K-channel subfamily K blocker | 46386821 | (4, 90, 120) | NIHCC Plate_5_H10 |
| Nitazoxanide | Decreased migration | Pyruvate-flavodoxin oxidoreductase inhibitor | 46386689 | (13, 49) | NIHCC Plate_6_A6 |
| 5-Cyclopropyl-1-(2-methoxypropyl)-5-methyl-2-phenylpiperazine | Decreased migration | Unknown | 104170212 | N/A | NIHCC Plate_7_D5 |
| 8-tert-butyl-6-(2-methoxypropyl)-6,9-diazaspiro[4.5]decane | Decreased migration | Unknown | 104170115 | N/A | NIHCC Plate_7_A10 |
| Felodipine | Decreased migration | Ca-channel blocker, inhibition of mineralocorticoid receptor, PDE1A/1B inhibitor | 104170219 | (21, 30, 35, 67, 100, 107a) | NIHCC Plate_7_C5 |
| Albendazole | Decreased migration | Tubulin-alpha/beta chain polymerization inhibition | 104170113 | (23, 92, 105) | NIHCC Plate_7_C9 |
| Azathioprine | Decreased migration | Inhibitor of hypoxanthine-guanine phosphoribosyl transferase | 104170112 | (6, 32) | NIHCC Plate_7_D9 |
| Griseofulvin | Decreased migration | Tubulin-alpha/beta chain polymerization inhibition | 104170114 | (55, 87), | NIHCC Plate_7_D10 |
| Miconazole | Decreased migration | Lanosterol 14-alpha demethylase inhibitor, K voltage-gated channel subfamily H inhibitor, Ca-activated K channel inhibitor | 104169959 | (3, 116) | NIHCC Plate_7_E3 |
| Daunorubicin | Decreased migration | DNA-topoisomerase-2 inhibitor | 104170197 | (10, 123) | NIHCC Plate_7_E7 |
| Minocycline | Decreased migration | Caspase-1 and -3 negative modulator, VEGF inhibitor, matrixmetalloproteinase-9 inhibitor, 16 rRNA inhibitor | 104169958 | (19, 31, 55, 87, 95, 109, 118) | NIHCC Plate_ |
| Mobendazole | Decreased migration | Tubulin-alpha/beta chain polymerization inhibition | 104170137 | (72, 85) | NIHCC Plate_8_A8 |
| Digoxin | Decreased migration | Na-K-ATPase inhibitor | 104170057 | (1) | NIHCC Plate_8_G5 |
| 5-Azacytidine | Decreased migration | DNA-methyltransferase 1 inhibitor | 104170170 | (24, 83), | NIHCC Plate_9_A10 |
| Podofilox | Decreased migration | Tubulin-alpha/beta chain polymerization inhibition, DNA-topoisomerase-2 inhibitor | 104170173 | (54, 59) | NIHCC Plate_9_C8 |
| Mitoxantrone | Decreased migration | DNA intercalation, DNA-topoisomerase-2 inhibitor | 104170122 | (21, 44) | NIHCC Plate_9_E5 |
| 1-(2-Methoxypropyl)-2,5,5-trimethyl-2-phenylpiperazine | Decreased migration | N/A | 104170092 | N/A | NIHCC Plate_10_B3 |
Preliminary hits ordered in ascending order from NIHCC plate. Fifty-seven of 61 positive results decreased migration and 4 increased (*) migration. All positive hits were screened in triplicate at 10 µM concentration and compared with a vehicle control (0.1% DMSO). NIHCC, National Institutes of Health Clinical Collection; PMR, podocyte migration rate; NMJ, neuromuscular junction; hERG, human ether-a-go-go-related gene; NSAID, nonsteroidal anti-inflammatory drugs; CNS, central nervous system; GI, gastrointestional; ACE, angiotensin-converting enzyme; COX, cyclooxygenase; Pubchem ID: https://pubchem.ncbi.nlm.nih.gov/.