Table 1. Cryo-EM structures of Na v... | Rockefeller University Press

Table 1.

Cryo-EM structures of Na_v channels with pore-blocking inhibitors resolved

PDB ID	Emd ID	Drug ID	Reference	Drug name	Drug Qscores	Ave.pore Qscores	Subtype
7W77	32341	966	Li et al. (2022)	Bulleyaconitine A	0.391	0.52	Human Na_v1.3
7W7F	32343	8DE	Li et al. (2022)	ICA-121431	0.409	0.489	Human Na_v1.3
6UZ0	20949	K4D	Jiang et al. (2020)	Flecainide^{^a}	0.557	0.527	rat Na_v1.5
6LQA	942	QDN	Li et al. (2021)	Quinidine	0.529	0.523	Human Na_v1.5
7FBS	31519	4Y4	Jiang et al. (2021)	Propafenone	0.556	0.57	rat Na_v1.5
8F6P	28887	XHO	Lenaeus et al. (2023)	Ranolazine	0.512	0.556	rat Na_v1.5
8T6L	41071	YIJ	Tonggu et al. (2024)	Batrachotoxin, Analog BTX-B	0.253, 0.31	0.545	rat Na_v1.5
7XM9	33292	G2E	Zhang et al. (2022)	XEN-907	0.483	0.541	Human Na_v1.7
7XMF	33295	G2W	Zhang et al. (2022)	IN2	0.463	0.563	Human Na_v1.7
7XMG	33296	G4I	Zhang et al. (2022)	TCN-1752	0.57	0.542	Human Na_v1.7
8I5B	35193	OJ0	Wu et al. (2023)	Bupivacaine	0.4	0.634	Human Na_v1.7
8I5G	35194	T70	Wu et al. (2023)	PF-05089771	0.64	0.647	Human Na_v1.7
8I5X	35197	T7F	Wu et al. (2023)	Vinpocetine	0.494	0.604	Human Na_v1.7
8I5Y	35198	TB4	Wu et al. (2023)	Vixotrigine	0.577	0.657	Human Na_v1.7
8J4F	35975	UK0	Wu et al. (2023)	Hardwickii acid	0.555	0.594	Human Na_v1.7
8S9B	40238	LQO	Wu et al. (2023)	Lacosamide^{^a}	0.665, 0.534	0.596	Human Na_v1.7
8S9C	40239	N6W	Wu et al. (2023)	Carbamazepine	0.56	0.577	Human Na_v1.7
8G1A	29665	P0T	Huang et al. (2023a)	Cannabidiol	0.491, 0.364	0.573	Human Na_v1.7
8THH	41262	IYJ	Huang et al. (2023b)	Lamotrigine^{^a}	0.589, 0.456	0.615	Human Na_v1.7
8THG	41261	657	Huang et al. (2023b)	Riluzole^{^a}	0.582	0.584	Human Na_v1.7
7WE4	32439	95T	Huang et al. (2022)	A-803467	0.659	0.609	Human Na_v1.8

PDB ID	Emd ID	Drug ID	Reference	Drug name	Drug Qscores	Ave.pore Qscores	Subtype
7W77	32341	966	Li et al. (2022)	Bulleyaconitine A	0.391	0.52	Human Na_v1.3
7W7F	32343	8DE	Li et al. (2022)	ICA-121431	0.409	0.489	Human Na_v1.3
6UZ0	20949	K4D	Jiang et al. (2020)	Flecainide^{^a}	0.557	0.527	rat Na_v1.5
6LQA	942	QDN	Li et al. (2021)	Quinidine	0.529	0.523	Human Na_v1.5
7FBS	31519	4Y4	Jiang et al. (2021)	Propafenone	0.556	0.57	rat Na_v1.5
8F6P	28887	XHO	Lenaeus et al. (2023)	Ranolazine	0.512	0.556	rat Na_v1.5
8T6L	41071	YIJ	Tonggu et al. (2024)	Batrachotoxin, Analog BTX-B	0.253, 0.31	0.545	rat Na_v1.5
7XM9	33292	G2E	Zhang et al. (2022)	XEN-907	0.483	0.541	Human Na_v1.7
7XMF	33295	G2W	Zhang et al. (2022)	IN2	0.463	0.563	Human Na_v1.7
7XMG	33296	G4I	Zhang et al. (2022)	TCN-1752	0.57	0.542	Human Na_v1.7
8I5B	35193	OJ0	Wu et al. (2023)	Bupivacaine	0.4	0.634	Human Na_v1.7
8I5G	35194	T70	Wu et al. (2023)	PF-05089771	0.64	0.647	Human Na_v1.7
8I5X	35197	T7F	Wu et al. (2023)	Vinpocetine	0.494	0.604	Human Na_v1.7
8I5Y	35198	TB4	Wu et al. (2023)	Vixotrigine	0.577	0.657	Human Na_v1.7
8J4F	35975	UK0	Wu et al. (2023)	Hardwickii acid	0.555	0.594	Human Na_v1.7
8S9B	40238	LQO	Wu et al. (2023)	Lacosamide^{^a}	0.665, 0.534	0.596	Human Na_v1.7
8S9C	40239	N6W	Wu et al. (2023)	Carbamazepine	0.56	0.577	Human Na_v1.7
8G1A	29665	P0T	Huang et al. (2023a)	Cannabidiol	0.491, 0.364	0.573	Human Na_v1.7
8THH	41262	IYJ	Huang et al. (2023b)	Lamotrigine^{^a}	0.589, 0.456	0.615	Human Na_v1.7
8THG	41261	657	Huang et al. (2023b)	Riluzole^{^a}	0.582	0.584	Human Na_v1.7
7WE4	32439	95T	Huang et al. (2022)	A-803467	0.659	0.609	Human Na_v1.8

Q-scores were extracted from Electron Microscopy Data Bank (https://www.ebi.ac.uk/emdb/) validation reports. Q-scores are used as a measure of resolvability in regions of a cryo-EM map – smaller the q-score, the lower the resolvability.

Indicates the instances where the averaged q-score of the surrounding pore residues is lower than the drug’s q-score. Bold indicates drug molecules not bound in the pore, but rather identified below the intracellular gate.

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