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Assay Detail

CHEMBL821404

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

Binding
Competition with [1251]L-692,884 for binding to purified alpha IIb/beta3 integrin, activated by coating onto yttrium silicate scintillation proximity assay fluomicrospheres.
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Integrin alpha-IIb/beta-3 (CHEMBL2093869)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors.
Egbertson MS, Bednar B, Askew BC, Bednar RA, Brashear K, Breslin MJ, Duggan ME, Fisher TE, Halczenko W, Hutchinson JH, Ihle N, Prugh JD, Wai JS, Gould RJ, Hartman GD.
Bioorg Med Chem Lett (2000) 10 : 1943 -1948
PubMed 10987423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 28 8.85 10.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL57040 1 10.25
CHEMBL298655 1 10.10
CHEMBL293601 1 10.05
CHEMBL59562 1 9.80
CHEMBL58328 1 9.60
CHEMBL298589 1 9.60
CHEMBL57191 1 9.59
CHEMBL293588 1 9.52
CHEMBL58713 1 9.47
CHEMBL57881 1 9.42
CHEMBL57886 1 9.25
CHEMBL58675 1 9.11
CHEMBL57192 1 9.11
CHEMBL58790 1 9.11
CHEMBL262194 1 9.07
CHEMBL292663 1 9.07
CHEMBL916 TIROFIBAN 4.0 1 8.72
CHEMBL59020 1 8.66
CHEMBL48371 1 8.35
CHEMBL57134 1 8.17
CHEMBL444573 1 8.05
CHEMBL58152 1 8.01
CHEMBL61353 1 7.92
CHEMBL32960 1 7.89
CHEMBL57094 1 7.82
CHEMBL441438 1 7.68
CHEMBL300097 1 7.34
CHEMBL58618 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL57040 Kd = 0.056 nM 10.25
CHEMBL298655 Kd = 0.08 nM 10.10
CHEMBL293601 Kd = 0.09 nM 10.05
CHEMBL59562 Kd = 0.16 nM 9.80
CHEMBL58328 Kd = 0.25 nM 9.60
CHEMBL298589 Kd = 0.25 nM 9.60
CHEMBL57191 Kd = 0.26 nM 9.59
CHEMBL293588 Kd = 0.3 nM 9.52
CHEMBL58713 Kd = 0.34 nM 9.47
CHEMBL57881 Kd = 0.38 nM 9.42
CHEMBL57886 Kd = 0.56 nM 9.25
CHEMBL58675 Kd = 0.77 nM 9.11
CHEMBL57192 Kd = 0.78 nM 9.11
CHEMBL58790 Kd = 0.78 nM 9.11
CHEMBL262194 Kd = 0.85 nM 9.07
CHEMBL292663 Kd = 0.86 nM 9.07
CHEMBL916 TIROFIBAN Kd = 1.9 nM 8.72
CHEMBL59020 Kd = 2.2 nM 8.66
CHEMBL48371 Kd = 4.5 nM 8.35
CHEMBL57134 Kd = 6.7 nM 8.17
CHEMBL444573 Kd = 9.0 nM 8.05
CHEMBL58152 Kd = 9.7 nM 8.01
CHEMBL61353 Kd = 12.0 nM 7.92
CHEMBL32960 Kd = 13.0 nM 7.89
CHEMBL57094 Kd = 15.0 nM 7.82
CHEMBL441438 Kd = 21.0 nM 7.68
CHEMBL300097 Kd = 46.0 nM 7.34
CHEMBL58618 Kd = 64.0 nM 7.19