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Assay Detail

CHEMBL4150231

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

Binding
Binding affinity to human integrin alphaVbeta3 receptor using acetyl-CisoDGRCGVRSSSRTPSDKY-bio probe and streptavidin-peroxidase conjugate incubated for 3 hrs by competitive binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Intermediate

Target

Integrin alpha-V/beta-3 (CHEMBL1907598)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Succinimide-Based Conjugates Improve IsoDGR Cyclopeptide Affinity to αvβ3 without Promoting Integrin Allosteric Activation.
Nardelli F, Paissoni C, Quilici G, Gori A, Traversari C, Valentinis B, Sacchi A, Corti A, Curnis F, Ghitti M, Musco G.
J Med Chem (2018) 61 : 7474 -7485
PubMed 29883545 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.86 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429876 CILENGITIDE 3.0 1 9.00
CHEMBL4161189 1 8.20
CHEMBL4168458 1 7.70
CHEMBL4165038 1 7.67
CHEMBL4160559 1 7.58
CHEMBL4171425 1 6.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429876 CILENGITIDE Ki = 1.0 nM 9.00
CHEMBL4161189 Ki = 6.3 nM 8.20
CHEMBL4168458 Ki = 19.9 nM 7.70
CHEMBL4165038 Ki = 21.6 nM 7.67
CHEMBL4160559 Ki = 26.5 nM 7.58
CHEMBL4171425 Ki = 103.0 nM 6.99