Table 8. Chemical Structures and Functional as Well as Binding Data for Willardiine Analogues 8.1−8.6^a.

cmpd	GluA2	GluK1	GluK2	GluK3	GluK1/2	GluK1/5	GluK2/5
8.1 (UBP282)b	−h	9.3	>1000d	−h	−h	−h	>1000d
8.2 (UBP296)c	>300	0.6	>1000d	>100d	0.8	1.0	>100d
8.3 (UBP302)e	>300	0.6	>100	4.0f	0.8	1.0	>300
8.4 (UBP304)e	>100	0.12	>100	−h	0.12	0.18	>100
8.5 (UBP310)e	>100	0.010	>100	0.023f	−h	0.008	>100
8.6 (ACET)e	>100	0.007g	>100	0.092f	−h	0.005	>100

^aAll values in [μM].

^bFrom ref (93): K_D values for inhibition of KA-induced currents in neonatal rat dorsal root C fibers.

^cK_B values for inhibition of 10−100 μM glutamate-induced Ca²⁺ influx in HEK 293 cells expressing human homomeric AMPA or KA receptor subtypes; from ref (95).

^dFrom ref (93): Binding study K_i or IC₅₀ from displacement of [³H]KA at human homomeric KA receptors expressed in HEK 293 cells.

^eFrom ref (91): K_i or IC₅₀ value for inhibition of glutamate-evoked currents in HEK 293 cells expressing homomeric KA receptors.

^fFrom ref (52): IC₅₀ values in an Xenopus oocyte assay.

^gIn another study, this value was measured to be 0.0014l; ref (100).

^hNot tested.