Table 3.

Peptide inhibitors targeting interactions mediated by Spike RBD on SARS‐CoV and SARS‐CoV‐2

Peptide name	Target	Sequence	Development Stage	Efficacy and/or binding kinetics b)
SARS‐CoV
P6[ 152 ]	RBD	EEQAKTFLDKFNHEAEDLFYQSSGLGKGDFR	In vitro	IC50 (P) = 0.1 µm
HR2‐8[ 81 ]	HR1	ELDSFKEELDKYFKNHTSPDVDLGDISGINASVVNIQKEIDRLNEVAKNLNESLIDLQELGKYEQYIK	In vitro	EC50 (V) = 17 µm
CP‐1[ 144 ]	HR1	GINASVVNIQKEIDRLNEVAKNLNESLIDLQELGKYE	In vitro	IC50 (V) = 19 µm
HR1‐1[ 165 ]	HR2	NGIGVTQNVLYENQKQIANQFNKAISQIQESLTTTSTA	In vitro	EC50 (V) = 3.68 µm
HR2‐18[ 165 ]	HR1	IQKEIDRLNEVAKNLNESLIDLQELGK	In vitro	EC50 (V) = 5.22 µm
HR2‐38[ 187 ]	HR1	GDISGINASVVNIQKEIDRLNEVAKNLNESLIDLQELGKYE	In vitro	IC50 (V) = 5 nm
SR9[ 188 ]	HR1	ISGINASVVNIQKEIDRLNEVAKNLNESLIDLQEL	In vitro	EC50 (V) = 5 nm
HR1‐a[ 143 ]	HR2	YENQKQIANQFNKAISQIQESLTTTSTA	In vitro	EC50 (P) = 1.61 µm
GST‐removed‐HR2[ 143 ]	HR1	DVDLGDISGINASVVNIQKEIDRLNEVAKNLNESLIDLQELGKYEQYI	In vitro	EC50 (P) = 2.15 µm
HR2[ 143 ]	HR1	ISGINASVVNIQKEIDRLNEVAKNLNESLIDLQEL	In vitro	EC50 (P) = 0.34 µm
P6[ 170 ]	HR1	GINASVVNIQKEIDRLNEVAKNL	In vitro	IC50 (V) = 2.28 µm
S471‐503[ 180 ]	ACE‐2	ALNCYWPLNDYGFYTTTGIGYQPYRVVVLSFEL	In vitro	EC50 (V) = 41.6 µm
SP‐10[ 221 ]	ACE‐2	STSQKSIVAYTM	In vitro	IC50 (B) = 1.88 nm
SARS‐CoV‐2
SBP‐1[ 150 ]	RBD	IEEQAKTFLDKFNHEAEDLFYQS	In vitro	K D (L) = 47 nm
Inhibitor 1[ 147 ]	RBD	IEEQAKTFLDKFNHEAEDLFYQSSLASWNYNTNIT	In silico	N/A
18 AA Peptide[ 151 ]	RBD	FLDKFNHEAEDLFYQSSL	In silico	N/A
SPB25F8N [ 137 ]	RBD	IEEQAKTNLDKFNHEAEDLFYQSSL	In silico	N/A
SPB25F8N/L25R [ 137 ]	RBD	IEEQAKTNLDKFNHEAEDLFYQSSR	In silico	N/A
SPB25L25V [ 137 ]	RBD	IEEQAKTFLDKFNHEAEDLFYQSSV	In silico	N/A
AVP0671[ 222 ]	RBD	TWLATRGLLRSPGRYVYFSPSASTWPVGIWTTGELVLGCDAAL	In silico	N/A
Peptide 1[ 223 ]	RBD	TVFGLNVWKRYSK‐(βA)‐K(Biotin)‐CONH2	In vitro	K D (L) = 250 nm
AVP1244[ 222 ]	ACE‐2	GCASRCKAKCAGRRCKGWASAFRGRCYCKCFRC	In silico	N/A
P8[ 171 ]	RBD	SALEEQLKTFLDKFMHELEDLLYQLAL	In vitro	IC50 (V) = 46 nm
P9[ 171 ]	RBD	SALEEQYKTFLDKFMHELEDLLYQLSL a)	In vitro	IC50 (V) = 53 nm
P10[ 171 ]	RBD	SALEEQYKTFLDKFMHELEDLLYQLAL a)	In vitro	IC50 (V) = 42 nm
AHB1[ 177 ]	RBD	DEDLEELERLYRKAEEVAKEAKDASRRGDDERAKEQMERAMRLFDQVFELAQELQEKQTDGNRQKATHLDKAVKEAADELYQRVR	In vitro	IC50 (V) = 35 nm
AHB2[ 177 ]	RBD	ELEEQVMHVLDQVSELAHELLHKLTGEELERAAYFNWWATEMMLELIKSDDEREIREIEEEARRILEHLEELARK	In vitro	IC50 (V) = 15.5 nm
LCB1[ 177 ]	RBD	DKEWILQKIYEIMRLLDELGHAEASMRVSDLIYEFMKKGDERLLEEAERLLEEVER	In vitro	IC50 (V) = 23.54 pm
LCB3[ 177 ]	RBD	NDDELHMLMTDLVYEALHFAKDEEIKKRVFQLFELADKAYKNNDRQKLEKVVEELKELLERLLS	In vitro	IC50 (V) = 48.1 pm
[22–44][ 224 ]	RBD	EEQAKTFLDKFNHEAEDLFYQSS	In vitro	IC50 = 1–10 µm
[22–57][ 224 ]	RBD	EEQAKTFLDKFNHEAEDLFYQSSLASWNYNTNITEE	In vitro	IC50 = 1–10 µm
2019‐nCoV HR2P[ 97 ]	HR1	DISGINASVVNIQKEIDRLNEVAKNLNESLIDLQEL	In vitro	IC50 (P) = 0.98 µm
EK1[ 96 ]	HR1	SLDQINVTFLDLEYEMKKLEEAIKKLEESYIDLKEL	In vitro	IC50 (P) = 2375 nm
EK1C4[ 96 ]	HR1	(N)EK1‐GSGSG‐PEG4‐(Chol)	In vitro	IC50 (P) = 15.8 nm
IPB02[ 148 ]	HR1	ISGINASVVNIQKEIDRLNEVAKNLNESLIDLQELK‐(Chol)	In vitro	IC50 (P) = 0.08 µm
[SARSHRC‐PEG4]2‐chol[ 225 ]	HR1	[DISGINASWNIQKEIDRLNEVAKNLNESLIDLQEL‐PEG4]2‐(Chol)	In vitro and in vivo	IC50 (V) = 3 nm
SARS‐BLOCK peptide 5[ 157 ]	ACE‐2	Unknown	In vitro	IC95 (P) = 6.66 µm
P9[ 171 ]	RBD	SALEEQYKTFLDKFMHELEDLLYQLSL	In vitro	IC50 (V) = 53 nm
P10[ 171 ]	RBD	SALEEQYKTFLDKFMHELED LLYQL AL	In vitro	IC50 (V) = 42 nm
RBD‐pep2[ 171 ]	RBD	IYQAGSTPCNGVEGFNCYFP	In vitro	N/A
DP7[ 172 ]	RBD	VQWRIRVAVIRK	In vitro	IC50 (P) = 73.625 µg mL−1
hACE221‐55A36K‐F40E[ 173 ]	RBD	IEEQAKTFLDKFNHEKEDLEYQSSLASWNYNTNIT	In vitro	IC50 (B) = 3.6 µm
SAP1[ 174 ]	RBD	TFLDKFNHEAEDLFYQ	In vitro	IC50 (P) = 2.39 mm
SAP2[ 175 ]	RBD	EDLFYQSSL	In vitro	IC50 (P) = 3.72 mm
SAP6[ 175 ]	RBD	EDLFYQ	In vitro	IC50 (P) = 1.90 mm

Note:

^a) is homotyrosine;

^b) V: Virus infection inhibition assay result; P: pseudotype virus with reporter inhibition assay result; B: competitive biotinylated enzyme‐linked immunosorbent assay (ELISA) of Spike protein and ACE‐2 result; L: bio‐layer interferometry (BLI). For BLI/SPR experiments, K _D is reported. EC₅₀ and IC₅₀, while representing the same value in this inhibition assay, are shown as initially reported.