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Assay Detail

CHEMBL5553091

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to biotinylated KRAS G12D mutant (unknown origin) incubated for 120 mins by SPR analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

GTPase KRas (CHEMBL2189121)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of middle-size cyclic peptides, KRAS inhibitors derived from an mRNA display.
Kage M, Hayashi R, Matsuo A, Tamiya M, Kuramoto S, Ohara K, Irie M, Chiyoda A, Takano K, Ito T, Kotake T, Takeyama R, Ishikawa S, Nomura K, Furuichi N, Morita Y, Hashimoto S, Kawada H, Nishimura Y, Nii K, Sase H, Ohta A, Kojima T, Iikura H, Tanada M, Shiraishi T.
Bioorg Med Chem (2024) 110 : 117830 -117830
PubMed 38981216 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 13 9.45 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5573020 1 9.85
CHEMBL5562993 1 9.80
CHEMBL5572821 1 9.77
CHEMBL5570195 1 9.74
CHEMBL5569602 1 9.72
CHEMBL5575367 1 9.64
CHEMBL5576025 1 9.59
CHEMBL5570375 1 9.49
CHEMBL5565237 1 9.33
CHEMBL5572706 1 9.19
CHEMBL5591865 1 9.12
CHEMBL5569112 1 8.96
CHEMBL5566631 1 8.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5573020 Kd = 0.14 nM 9.85
CHEMBL5562993 Kd = 0.16 nM 9.80
CHEMBL5572821 Kd = 0.17 nM 9.77
CHEMBL5570195 Kd = 0.18 nM 9.74
CHEMBL5569602 Kd = 0.19 nM 9.72
CHEMBL5575367 Kd = 0.23 nM 9.64
CHEMBL5576025 Kd = 0.26 nM 9.59
CHEMBL5570375 Kd = 0.32 nM 9.49
CHEMBL5565237 Kd = 0.47 nM 9.33
CHEMBL5572706 Kd = 0.64 nM 9.19
CHEMBL5591865 Kd = 0.75 nM 9.12
CHEMBL5569112 Kd = 1.1 nM 8.96
CHEMBL5566631 Kd = 2.5 nM 8.60