Table 7Analogues with R1 – R4 substitution patterns in combination
Entry | SID/CID | * | Efflux Assay Potency (μM) mean (n = # replicates) | Selectivity B1:G2 | Potentiation Assays | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
R1 | R2 | R3 | R4 | ABC B1 | ABC G2 | ABC B1 | ABC G2 | ||||||||||
n | IC50 μM (% Res)a | n | IC50 μM (% Res)a | CR50 (μM) | TD50 (μM) | TD50/ CR50 | CR50 (μM) | TD50 (μM) | TD50/ CR50 | ||||||||
1 | SID88095709 | S | phenyl | 2-furyl | H | CO-3- furan | 5 | 4.65 (112) | 4 | 0.13 (98) | 35.8 | 0.55 | 5.52 | toxic | 0.31 | 18.30 | 59 |
CID44640177 | |||||||||||||||||
2 | SID99376136 | S | 3-Cl-phenyl | 2-furyl | H | COCH3 | 1 | 0.80 (113) | 2 | 0.56 (127) | 1.4 | 0.08 | 17.60 | 232 | 0.58 | >100 | 174 |
CID46912089 | |||||||||||||||||
3 | SID99376137 | S | 3-MeO-phenyl | 2-furyl | H | COCH3 | 1 | 1.64 (66) | 2 | 1.9 (121) | 0.9 | 0.32 | 49.30 | 155 | 1.18 | >100 | 85 |
CID46912090 | |||||||||||||||||
4 | SID99376134 | S | 4-Me-phenyl | 2-furyl | H | CH2-3- furan | 1 | 8.7 (114) | 2 | 2.67 (64) | 3.3 | 0.35 | 12.50 | toxic | 1.68 | 57.80 | 34 |
CID46912091 | |||||||||||||||||
5 | SID87557810 | S | phenyl | methyl | methyl | CO-3- furan | 5 | 1.63 (33) | 5 | 2.18 (94) | 0.7 | NT | NT | NT | NT | ||
CID44629743 | |||||||||||||||||
6 | SID97301789 | S | 3-MeO-phenyl | methyl | methyl | CH2-3- furan | 3 | 50.00 | 4 | 0.21 (82) | 233.2 | 0.02 | >100 | 5495 | 0.09 | >100 | 1176 |
CID46245505 |
- a
Percent Response;
- *
S = synthesized; P = purchased; NT = not tested
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- Table 7, Analogues with R1 – R4 substitution patterns in combination - Probe Rep...Table 7, Analogues with R1 – R4 substitution patterns in combination - Probe Reports from the NIH Molecular Libraries Program
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