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Assay Detail

CHEMBL3784478

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

Binding
Competitive inhibition of human coagulation factor 11a assessed as reduction in release of p-nitroaniline after 10 to 120 mins by Michaelis-Menten equation analysis
32
Total Activities
32
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 pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.
Corte JR, Fang T, Pinto DJ, Orwat MJ, Rendina AR, Luettgen JM, Rossi KA, Wei A, Ramamurthy V, Myers JE, Sheriff S, Narayanan R, Harper TW, Zheng JJ, Li YX, Seiffert DA, Wexler RR, Quan ML.
Bioorg Med Chem (2016) 24 : 2257 -2272
PubMed 27073051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 7.86 9.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3398612 1 9.51
CHEMBL3781742 1 8.62
CHEMBL3780342 1 8.62
CHEMBL3781202 1 8.49
CHEMBL3780324 1 8.43
CHEMBL3780922 1 8.42
CHEMBL3781553 1 8.28
CHEMBL3781788 1 8.20
CHEMBL3398642 1 8.17
CHEMBL3781363 1 8.17
CHEMBL3393386 1 8.14
CHEMBL3780189 1 8.12
CHEMBL3780777 1 8.10
CHEMBL3780030 1 8.08
CHEMBL3781550 1 8.04
CHEMBL3780285 1 8.04
CHEMBL3781505 1 8.00
CHEMBL3780001 1 7.96
CHEMBL3781580 1 7.92
CHEMBL3393385 1 7.89
CHEMBL3780127 1 7.77
CHEMBL3781319 1 7.64
CHEMBL3781277 1 7.62
CHEMBL3780751 1 7.28
CHEMBL3781981 1 7.25
CHEMBL3780930 1 7.21
CHEMBL3780501 1 7.06
CHEMBL3781679 1 7.06
CHEMBL3781581 1 7.01
CHEMBL3781691 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3398612 Ki = 0.31 nM 9.51
CHEMBL3781742 Ki = 2.4 nM 8.62
CHEMBL3780342 Ki = 2.4 nM 8.62
CHEMBL3781202 Ki = 3.197 nM 8.49
CHEMBL3780324 Ki = 3.7 nM 8.43
CHEMBL3780922 Ki = 3.8 nM 8.42
CHEMBL3781553 Ki = 5.3 nM 8.28
CHEMBL3781788 Ki = 6.3 nM 8.20
CHEMBL3398642 Ki = 6.7 nM 8.17
CHEMBL3781363 Ki = 6.7 nM 8.17
CHEMBL3393386 Ki = 7.2 nM 8.14
CHEMBL3780189 Ki = 7.5 nM 8.12
CHEMBL3780777 Ki = 7.9 nM 8.10
CHEMBL3780030 Ki = 8.4 nM 8.08
CHEMBL3780285 Ki = 9.2 nM 8.04
CHEMBL3781550 Ki = 9.1 nM 8.04
CHEMBL3781505 Ki = 10.0 nM 8.00
CHEMBL3780001 Ki = 11.0 nM 7.96
CHEMBL3781580 Ki = 12.0 nM 7.92
CHEMBL3393385 Ki = 13.0 nM 7.89
CHEMBL3780127 Ki = 17.0 nM 7.77
CHEMBL3781319 Ki = 23.0 nM 7.64
CHEMBL3781277 Ki = 24.0 nM 7.62
CHEMBL3780751 Ki = 53.0 nM 7.28
CHEMBL3781981 Ki = 56.0 nM 7.25
CHEMBL3780930 Ki = 61.0 nM 7.21
CHEMBL3780501 Ki = 87.0 nM 7.06
CHEMBL3781679 Ki = 87.0 nM 7.06
CHEMBL3781581 Ki = 97.0 nM 7.01
CHEMBL3781691 Ki = 110.0 nM 6.96
CHEMBL3781468 Ki = 144.0 nM 6.84
CHEMBL3780389 Ki = 205.0 nM 6.69