Table 1 KM12 and KM12-AM affinity profiling to different RAS proteins

From: Identification and characterization of binders to a cryptic and functional pocket in KRAS

KD (mean ± SD in nM)

KRAS

NRAS

HRAS

WT

G12D

Q61R

WT

Q61R

WT

GDP

GMPPnP

GDP

GMPPnP

GTP

GDP

GMPPnP

GTP

GDP

GMPPnP

KM12

190 ± 134

300/340

90/100

300/330

370

1060 ± 787

1820/1420

2020

420 ± 165

530/920

KM12-AM

7.9 ± 2

4.8/10

6.7 ± 1

4.8/10

12

22 ± 1

14/15

24

10 ± 1

8/8.8

  1. The indicated WT and mutant H- and N- KRAS proteins were fully loaded either with GDP or the non-hydrolyzable GTP-analog GMPPnP. As NRASQ61R displays a strongly impaired intrinsic hydrolysis, it allowed for assessment of the GTP-loaded state. SPR determined KD’s are represented as n ≥ 4 independent experiments mean ± SD, or as individual values when only n = 2 determinations were performed. Source Data are provided as a source Data file.
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