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Assay Detail

CHEMBL685829

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

Binding
Ability to inhibit binding of biotin-labeled human fibrinogen to immobilized fibrinogen receptor purified from human erythroleukemia (HEL) cells.
32
Total Activities
32
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

Novel non-peptide fibrinogen receptor antagonists. 1. Synthesis and glycoprotein IIb-IIIa antagonistic activities of 1,3,4-trisubstituted 2-oxopiperazine derivatives incorporating side-chain functions of the RGDF peptide.
Sugihara H, Fukushi H, Miyawaki T, Imai Y, Terashita Z, Kawamura M, Fujisawa Y, Kita S.
J Med Chem (1998) 41 : 489 -502
PubMed 9484499 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 8.02 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL145956 1 9.68
CHEMBL344544 1 9.54
CHEMBL147976 1 9.38
CHEMBL310081 1 9.31
CHEMBL146979 1 9.05
CHEMBL450621 1 9.04
CHEMBL148010 1 9.04
CHEMBL118402 1 9.00
CHEMBL146627 1 9.00
CHEMBL444861 1 8.80
CHEMBL146393 1 8.71
CHEMBL422486 1 8.60
CHEMBL356363 1 8.32
CHEMBL146784 1 8.21
CHEMBL146031 1 8.09
CHEMBL146523 1 7.82
CHEMBL146417 1 7.79
CHEMBL147921 1 7.75
CHEMBL149424 1 7.75
CHEMBL358154 1 7.70
CHEMBL341673 1 7.70
CHEMBL146721 1 7.68
CHEMBL145986 1 7.43
CHEMBL422132 1 7.35
CHEMBL356739 1 7.34
CHEMBL344506 1 7.20
CHEMBL423391 1 6.96
CHEMBL146323 1 6.89
CHEMBL265628 1 6.75
CHEMBL436405 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL145956 IC50 = 0.21 nM 9.68
CHEMBL344544 IC50 = 0.29 nM 9.54
CHEMBL147976 IC50 = 0.42 nM 9.38
CHEMBL310081 IC50 = 0.49 nM 9.31
CHEMBL146979 IC50 = 0.89 nM 9.05
CHEMBL450621 IC50 = 0.91 nM 9.04
CHEMBL148010 IC50 = 0.92 nM 9.04
CHEMBL118402 IC50 = 1.0 nM 9.00
CHEMBL146627 IC50 = 1.0 nM 9.00
CHEMBL444861 IC50 = 1.6 nM 8.80
CHEMBL146393 IC50 = 1.95 nM 8.71
CHEMBL422486 IC50 = 2.5 nM 8.60
CHEMBL356363 IC50 = 4.8 nM 8.32
CHEMBL146784 IC50 = 6.1 nM 8.21
CHEMBL146031 IC50 = 8.1 nM 8.09
CHEMBL146523 IC50 = 15.0 nM 7.82
CHEMBL146417 IC50 = 16.4 nM 7.79
CHEMBL147921 IC50 = 18.0 nM 7.75
CHEMBL149424 IC50 = 18.0 nM 7.75
CHEMBL358154 IC50 = 20.0 nM 7.70
CHEMBL341673 IC50 = 20.0 nM 7.70
CHEMBL146721 IC50 = 21.0 nM 7.68
CHEMBL145986 IC50 = 37.0 nM 7.43
CHEMBL422132 IC50 = 45.0 nM 7.35
CHEMBL356739 IC50 = 46.0 nM 7.34
CHEMBL344506 IC50 = 63.0 nM 7.20
CHEMBL423391 IC50 = 110.0 nM 6.96
CHEMBL146323 IC50 = 130.0 nM 6.89
CHEMBL265628 IC50 = 180.0 nM 6.75
CHEMBL436405 IC50 = 210.0 nM 6.68
CHEMBL148183 IC50 = 330.0 nM 6.48
CHEMBL147553 IC50 = 2630.0 nM 5.58