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Assay Detail

CHEMBL4056973

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

Binding
Inhibition of human Factor XIa using S-2366 as chromogenic substrate after 60 mins by Lineweaver-Burk plot analysis
29
Total Activities
25
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

Coagulation factor XI (CHEMBL2820)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency.
Corte JR, Yang W, Fang T, Wang Y, Osuna H, Lai A, Ewing WR, Rossi KA, Myers JE, Sheriff S, Lou Z, Zheng JJ, Harper TW, Bozarth JM, Wu Y, Luettgen JM, Seiffert DA, Quan ML, Wexler RR, Lam PYS.
Bioorg Med Chem Lett (2017) 27 : 3833 -3839
PubMed 28687203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 8.70 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4060950 1 10.52
CHEMBL4097522 1 10.22
CHEMBL4083769 1 10.15
CHEMBL4063677 1 9.89
CHEMBL4103982 1 9.85
CHEMBL4071545 1 9.80
CHEMBL4089185 1 9.74
CHEMBL4063746 2 9.48
CHEMBL4101766 1 9.41
CHEMBL4062923 1 9.33
CHEMBL4070961 1 9.16
CHEMBL3676167 1 9.00
CHEMBL4076558 1 8.96
CHEMBL4077140 1 8.70
CHEMBL4090854 1 8.49
CHEMBL3699199 2 8.23
CHEMBL4059590 2 8.19
CHEMBL4080459 1 8.15
CHEMBL4078696 1 8.00
CHEMBL4086540 1 7.92
CHEMBL4105168 1 7.80
CHEMBL4095227 1 7.68
CHEMBL4098046 1 7.68
CHEMBL4067808 2 7.46
CHEMBL4065103 1 7.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4060950 Ki = 0.03 nM 10.52
CHEMBL4097522 Ki = 0.06 nM 10.22
CHEMBL4083769 Ki = 0.07 nM 10.15
CHEMBL4063677 Ki = 0.13 nM 9.89
CHEMBL4103982 Ki = 0.14 nM 9.85
CHEMBL4071545 Ki = 0.16 nM 9.80
CHEMBL4089185 Ki = 0.18 nM 9.74
CHEMBL4063746 Ki = 0.33 nM 9.48
CHEMBL4101766 Ki = 0.39 nM 9.41
CHEMBL4062923 Ki = 0.47 nM 9.33
CHEMBL4070961 Ki = 0.69 nM 9.16
CHEMBL3676167 Ki = 1.0 nM 9.00
CHEMBL4076558 Ki = 1.1 nM 8.96
CHEMBL4077140 Ki = 2.0 nM 8.70
CHEMBL4063746 Ki = 2.7 nM 8.57
CHEMBL4090854 Ki = 3.2 nM 8.49
CHEMBL3699199 Ki = 5.9 nM 8.23
CHEMBL4059590 Ki = 6.5 nM 8.19
CHEMBL4080459 Ki = 7.0 nM 8.15
CHEMBL4078696 Ki = 10.0 nM 8.00
CHEMBL4086540 Ki = 12.0 nM 7.92
CHEMBL4105168 Ki = 16.0 nM 7.80
CHEMBL3699199 Ki = 18.0 nM 7.75
CHEMBL4095227 Ki = 21.0 nM 7.68
CHEMBL4098046 Ki = 21.0 nM 7.68
CHEMBL4059590 Ki = 31.0 nM 7.51
CHEMBL4067808 Ki = 35.0 nM 7.46
CHEMBL4067808 Ki = 36.0 nM 7.44
CHEMBL4065103 Ki = 44.0 nM 7.36