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Assay Detail

CHEMBL823497

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Binding
Inhibition of integrin alpha4-beta1 adhesion to Jurkat cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Jurkat
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Integrin alpha-4/beta-1 (CHEMBL1907599)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Selective, tight-binding inhibitors of integrin alpha4beta1 that inhibit allergic airway responses.
Lin K, Ateeq HS, Hsiung SH, Chong LT, Zimmerman CN, Castro A, Lee WC, Hammond CE, Kalkunte S, Chen LL, Pepinsky RB, Leone DR, Sprague AG, Abraham WM, Gill A, Lobb RR, Adams SP.
J Med Chem (1999) 42 : 920 -934
PubMed 10072689 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.80 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88478 1 8.40
CHEMBL1791268 1 8.30
CHEMBL369635 1 8.22
CHEMBL173699 1 8.10
CHEMBL275913 1 7.70
CHEMBL353994 1 7.52
CHEMBL173552 1 7.17
CHEMBL64387 1 6.70
CHEMBL354130 1 5.49
CHEMBL368564 1 5.30
CHEMBL355249 1 4.40
CHEMBL173870 1 4.29
CHEMBL172193 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88478 IC50 = 4.0 nM 8.40
CHEMBL1791268 IC50 = 5.0 nM 8.30
CHEMBL369635 IC50 = 6.0 nM 8.22
CHEMBL173699 IC50 = 8.0 nM 8.10
CHEMBL275913 IC50 = 20.0 nM 7.70
CHEMBL353994 IC50 = 30.0 nM 7.52
CHEMBL173552 IC50 = 68.0 nM 7.17
CHEMBL64387 IC50 = 200.0 nM 6.70
CHEMBL354130 IC50 = 3250.0 nM 5.49
CHEMBL368564 IC50 = 5000.0 nM 5.30
CHEMBL355249 IC50 = 40000.0 nM 4.40
CHEMBL173870 IC50 = 51000.0 nM 4.29
CHEMBL172193 IC50 = 175000.0 nM -