Table 2. One-Dose % of Glutaminase Activity Inhibition in the GAC–GDH–Diaphorase and GDH–Diaphorase Fluorescent Assays and the IC₅₀ and Reversibility Calculated with the GAC-GDH Absorbance Assay of the 11 Hit Compounds.

		fluorescent assay		absorbance assay
cpd	Chembridge ID #	% inhibition GAC–GDH–diaph.	% inhib. GDH–diaph.	IC50 (μM) GAC [95% CI]	IC50 (μM) KGA [95% CI]	reversibility (% recovered activity)
C1	7992402	73	1	11 [10–12]	11 [8–14]	1
C2	9155049	73	2	3 [2–4]	4 [3–4]	22
C3	7956101	69	–10	2 [2–3]	3 [3–4]	44
C4	9125354	69	–1	3 [2–3]	4 [3–4]	29
C5	7952342	68	–8	1 [0.9–1.2]	1.8 [1.6–2.1]	33
C6a	6744277	60	–7	>50	>50	66
C6b	5603967	57	–3	>50	>50	56
C7	5354303	60	–4	43 [37–48]	∼26	99
C8	7962214	58	–5	6 [5.6–6.3]	2.6 [2.4–2.7]	78
C9	9007737	50	–7	85 [73–99]	18 [13–25]	79
C10	7951061	48	–3	3 [2–5]	13 [11–15]	95
BPTES				0.08 [0.05–0.10]	0.18 [0.16–0.20]