Table 3.

Summary of the screening performed on human α6/3β2β3^V273S-nAChRs

	Number of compounds tested
	Total	Positive
SET		Single shota	Progressed to CRCb	pIC50 ≥ 6.0c	Hit rated	Number of chemotypese	Overlapf
Nicotinic	1 886	955	40	13	32.5	12	2
CNS	92 694	11 997	151	51	33.8	45	1
BFP	5 237	2 476	53	3	5.7	3	1

IC₅₀, concentration giving 50% of maximal inhibition; BFP, biological fingerprints; CNS, central nervous system.

^aCompounds giving ≥ 50% inhibition of nicotine-induced Ca²⁺ entrance at 10 µM (nicotinic and CNS set) or 20 µM (BFP set).

^bCompounds chosen for determination of activation and inhibition concentration response curves (CRC), according to the filtering criteria described in Materials and Methods.

^cCompounds inhibiting nicotine response with a pIC₅₀≥ 6.0 and unable to activate the receptors (pEC₅₀≤ 4.7).

^dPercentage of hits showing a pIC₅₀≥ 6.0, with respect to those progressed to concentration response curve determination.

^eNumber of clusters obtained with Ward cluster analysis of the pIC₅₀≥ 6.0 hits.

^fNumber of the pIC₅₀≥ 6.0 hits structurally similar to those of the other hit lists; similarity was assessed with Daylight fingerprints as descriptors and Tanimoto index greater or equal to 0.85.