Table 1 Scoring for the selection of the 3 confirmed hits

	Pre-selected hits^a	Score^b (safety)	Score^c (PK)	Score (total)
1	NITD609	3	6	9
2	(S)-(-)-Tetrahydropalmatine	3	6	9
3	TD-6450	3	3	6
4	MMV-390048	3	2	5
5	Halofuginone	3	1	4
6	Mitoquinone mesylate	3	1	4
7	Digitoxin	3	0	3
8	NVP-BGT226	0	2	2
9	KDU731	1	0	1
10	Chlorproguanil hydrochloride	0	1	1
11	Atiprimod dimaleate	0	0	0
12	Quisinostat	0	0	0
13	Abexinostat	0	0	0
14	Leuco methylthioninium salt	0	0	0
15	N-tert-butylisoquine	0	0	0
16	Auranofin	0	0	0
17	DDD498	0	0	0
18	AR-42	0	0	0
19	Paranyline	0	0	0
20	Ceritinib	0	0	0
21	Lanatoside A	0	0	0
22	Givinostat hydrochloride	0	0	0
23	CUDC-907	0	0	0
24	MLN 576	0	0	0
25	CHR-3996	0	0	0
26	Cymarine	0	0	0
27	Proscillaridin	0	0	0
28	Panobinostat lactate	0	0	0
29	Stilbazium iodide	0	0	0
30	YM 161514	0	0	0
31	Pirtenidine	0	0	0
32	BRD-7929	0	0	0

The 3 confirmed hits are in bold.
^a44 of the 76 DRA-confirmed hits from the ReFrame library (Fig. 1) were excluded because they were not orally administered to humans.
^bSerious adverse events reported in human subjects or no data available (Score = 0); Safe in animal models (Score = 1); No serious adverse events reported in human subjects (phase I or II) (Score = 3); No serious adverse events reported in human subjects (phase III or IV) (Score = 4).
^cData not available (Score = 0); Peak plasma concentration lower than 1/3 IC₅₀ (Score = 1); Peak plasma concentration between 1/3 IC₅₀ and IC₅₀ (Score = 2); Peak plasma concentration between IC₅₀ and 3 IC₅₀ (Score = 3); Peak plasma concentration higher than 3 IC₅₀ (Score = 6).

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