Table 2 Kinetic parameters of peptides. Both COLDER and SPR values show mean ± SEM from three independent replicates

From: Discovering covalent cyclic peptide inhibitors of peptidyl arginine deiminase 4 (PADI4) using mRNA-display with a genetically encoded electrophilic warhead

 

SPR

Colders

 

Ki (µM)

kinact (min-1)

kinact/Ki (M-1 min-1)

KI (µM)

kinact (min-1)

kinact/KI (M-1 min-1)

cP4_2

1.3 ± 0.5

0.12 ± 0.1

92,000

-

-

-

cP4_4

0.12 ± 0.01

0.11 ± 0.1

909,000

1.9 ± 0.1

0.13 ± 0.01

74,000

cP4_7

1.6 ± 0.1

0.55 ± 0.02

343,000

4.3 ± 1.1

0.077 ± 0.052

18,000

cP4_10

0.12 ± 0.1

0.23 ± 0.01

2,007,000

1.5 ± 0.3

0.13 ± 0.03

87,000

cP4_15

0.16 ± 0.03

0.25 ± 0.04

1,594,000

0.78 ± 0.06

0.17 ± 0.02

213,000

cP4_165

0.62 ± 0.06

0.066 ± 0.007

107,000

8.9 ± 1.1

0.16 ± 0.01

17,000

PADI4_3 H4(2)

0.015 ± 0.002

0.061 ± 0.011

4,083,000

1.1 ± 0.2

0.16 ± 0.03

149,000

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