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Assay Detail

CHEMBL4611642

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

Binding
Inhibition of recombinant human activated coagulation factor XI using pyro-Glu-Pro-Arg-pNA as substrate by spectrophotometry
25
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

Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa.
Fang T, Corte JR, Gilligan PJ, Jeon Y, Osuna H, Rossi KA, Myers JE, Sheriff S, Lou Z, Zheng JJ, Harper TW, Bozarth JM, Wu Y, Luettgen JM, Seiffert DA, Wexler RR, Lam PYS.
Bioorg Med Chem Lett (2020) 30 : 126949 -126949
PubMed 31932224 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 8.39 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4071545 1 9.80
CHEMBL3699175 1 9.66
CHEMBL4632633 1 9.51
CHEMBL4640111 1 9.34
CHEMBL3699176 1 9.21
CHEMBL4641689 1 9.17
CHEMBL3676167 1 9.00
CHEMBL4647704 1 8.96
CHEMBL4634088 1 8.89
CHEMBL4637778 1 8.70
CHEMBL4645389 1 8.60
CHEMBL4643121 1 8.59
CHEMBL4633349 1 8.47
CHEMBL4635313 1 8.44
CHEMBL4634869 1 8.29
CHEMBL4635248 1 8.22
CHEMBL4642584 1 8.08
CHEMBL4640474 1 7.92
CHEMBL3699163 1 7.80
CHEMBL4647369 1 7.80
CHEMBL4637252 1 7.62
CHEMBL4646216 1 7.32
CHEMBL4647199 1 7.28
CHEMBL3699189 1 6.61
CHEMBL4634680 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4071545 Ki = 0.16 nM 9.80
CHEMBL3699175 Ki = 0.22 nM 9.66
CHEMBL4632633 Ki = 0.31 nM 9.51
CHEMBL4640111 Ki = 0.46 nM 9.34
CHEMBL3699176 Ki = 0.61 nM 9.21
CHEMBL4641689 Ki = 0.67 nM 9.17
CHEMBL3676167 Ki = 1.0 nM 9.00
CHEMBL4647704 Ki = 1.1 nM 8.96
CHEMBL4634088 Ki = 1.3 nM 8.89
CHEMBL4637778 Ki = 2.0 nM 8.70
CHEMBL4645389 Ki = 2.5 nM 8.60
CHEMBL4643121 Ki = 2.6 nM 8.59
CHEMBL4633349 Ki = 3.4 nM 8.47
CHEMBL4635313 Ki = 3.6 nM 8.44
CHEMBL4634869 Ki = 5.1 nM 8.29
CHEMBL4635248 Ki = 6.0 nM 8.22
CHEMBL4642584 Ki = 8.3 nM 8.08
CHEMBL4640474 Ki = 12.0 nM 7.92
CHEMBL3699163 Ki = 16.0 nM 7.80
CHEMBL4647369 Ki = 16.0 nM 7.80
CHEMBL4637252 Ki = 24.0 nM 7.62
CHEMBL4646216 Ki = 48.0 nM 7.32
CHEMBL4647199 Ki = 53.0 nM 7.28
CHEMBL3699189 Ki = 245.0 nM 6.61
CHEMBL4634680 Ki = 370.0 nM 6.43