. Author manuscript; available in PMC: 2022 Feb 15.

Published in final edited form as: Bioorg Med Chem. 2021 Jan 8;32:116000. doi: 10.1016/j.bmc.2021.116000

Table 4.

Inhibitory activity of NBD-14273 against a large panel of FDA approved drug-resistant viruses

	NIH catalog#	Major mutations^a	NBD-14273 IC₅₀ (μM)^b	Fold increase/Se nsitive
NL4–3 WT (wild-type)	#114	-	0.21±0.04	-
ENTRY (Enfuvirtide)-resistant	#9498	V38A, N42T	0.4±0.08	1.9
	#9490	V38A	0.44±0.02	2.09
	#9496	V38E, N42S	0.31±0.03	1.48
	#9491	N42T, N43K	0.62±0.07	2.95
	#9489	D36G	0.34±0.06	1.62
Multi-drug (NNRTI)- resistant	#12227	K101P, K103N	0.11±0.006	Sensitive
	#12229	L100I, K103N	0.39±0.4	1.86
	#12231	K103N, Y181C	0.12±0.006	Sensitive
	#12233	K101E, Y181V	0.71±0.02	3.38
	#12237	Y181C, G190A	0.3±0.02	1.4
	#12239	K101E, E138K, Y181C	0.81±0.08	3.85
	#12241	K101E, G190S	0.26±0.01	Sensitive
	#12243	L100I, M230L	1.4±0.05	6.7
Integrase (Raltegravir-resistant)	#11847	G140S, Q148H	0.17±0.02	Sensitive
	#11850	E92Q, N155H	0.11±0.1	Sensitive
	#11851	N155H	0.12±0.01	Sensitive
	#11800	11I, 32I, 33F, 46I, 47V, 54M, 58E, 73S, 84V, 89V, 90M	0.1±0.01	Sensitive
	#11801	10F, 33F, 43T, 46L, 54V, 82A, 84V, 90M	0.12±0.02	Sensitive
	#11803	33F, 43T, 46I, 48V, 50V, 54S, 82A	0.38±0.1	1.8
	#11804	32I, 46I, 47V, 84V	0.24±0.02	Sensitive
	#11805	48V, 53L, 54V, 82A, 90M	0.16±0.05	Sensitive
	#11807	32I, 33F, 47A, 82A, 90M	0.12±0.03	Sensitive
	#11808	10F, 11I, 33F, 43T, 46L, 54V, 73S, 82A, 84V, 89V, 90M	0.17±0.03	Sensitive
	#12465	46I, 54V, 58E, 74P, 82L, 90M	0.13±0.02	Sensitive
	#12466	32I, 33F, 43T, 46I, 47V, 54M, 73S, 82A, 89V, 90M	0.11±0.02	Sensitive
	#12467		0.15±0.07	Sensitive

Mutants were reported here as per the data obtained from https://www.aidsreagent.org/ and associated references indicated in the Experimental Section.

The reported IC₅₀ values represent the means ± standard deviations (n = 3).