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Assay Detail

CHEMBL933439

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

Binding
Inhibition of human factor 10a
53
Total Activities
53
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 X (CHEMBL244)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Sulfonamidolactam inhibitors of coagulation factor Xa.
Smallheer JM, Wang S, Laws ML, Nakajima S, Hu Z, Han W, Jacobson I, Luettgen JM, Rossi KA, Rendina AR, Knabb RM, Wexler RR, Lam PY, Quan ML.
Bioorg Med Chem Lett (2008) 18 : 2428 -2433
PubMed 18329876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 53 8.16 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL270221 1 10.89
CHEMBL401958 1 10.80
CHEMBL256451 1 10.70
CHEMBL270862 1 10.70
CHEMBL270034 1 10.43
CHEMBL258274 1 10.37
CHEMBL269955 1 10.30
CHEMBL256820 1 10.00
CHEMBL271904 1 9.96
CHEMBL442457 1 9.89
CHEMBL401788 1 9.68
CHEMBL404119 1 9.46
CHEMBL402828 1 9.37
CHEMBL272136 1 9.15
CHEMBL256628 1 9.08
CHEMBL408044 1 9.06
CHEMBL271427 1 9.00
CHEMBL270829 1 8.96
CHEMBL270565 1 8.77
CHEMBL270255 1 8.66
CHEMBL403106 1 8.66
CHEMBL256890 1 8.64
CHEMBL272349 1 8.62
CHEMBL257854 1 8.57
CHEMBL402064 1 8.28
CHEMBL257037 1 8.00
CHEMBL429741 1 7.80
CHEMBL402237 1 7.75
CHEMBL429758 1 7.72
CHEMBL255799 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL270221 Ki = 0.013 nM 10.89
CHEMBL401958 Ki = 0.016 nM 10.80
CHEMBL270862 Ki = 0.02 nM 10.70
CHEMBL256451 Ki = 0.02 nM 10.70
CHEMBL270034 Ki = 0.037 nM 10.43
CHEMBL258274 Ki = 0.043 nM 10.37
CHEMBL269955 Ki = 0.05 nM 10.30
CHEMBL256820 Ki = 0.1 nM 10.00
CHEMBL271904 Ki = 0.11 nM 9.96
CHEMBL442457 Ki = 0.13 nM 9.89
CHEMBL401788 Ki = 0.21 nM 9.68
CHEMBL404119 Ki = 0.35 nM 9.46
CHEMBL402828 Ki = 0.43 nM 9.37
CHEMBL272136 Ki = 0.71 nM 9.15
CHEMBL256628 Ki = 0.84 nM 9.08
CHEMBL408044 Ki = 0.88 nM 9.06
CHEMBL271427 Ki = 1.0 nM 9.00
CHEMBL270829 Ki = 1.1 nM 8.96
CHEMBL270565 Ki = 1.7 nM 8.77
CHEMBL270255 Ki = 2.2 nM 8.66
CHEMBL403106 Ki = 2.2 nM 8.66
CHEMBL256890 Ki = 2.3 nM 8.64
CHEMBL272349 Ki = 2.4 nM 8.62
CHEMBL257854 Ki = 2.7 nM 8.57
CHEMBL402064 Ki = 5.3 nM 8.28
CHEMBL257037 Ki = 10.0 nM 8.00
CHEMBL429741 Ki = 16.0 nM 7.80
CHEMBL402237 Ki = 18.0 nM 7.75
CHEMBL429758 Ki = 19.0 nM 7.72
CHEMBL255799 Ki = 19.0 nM 7.72
CHEMBL272736 Ki = 23.0 nM 7.64
CHEMBL272115 Ki = 26.0 nM 7.58
CHEMBL403291 Ki = 28.0 nM 7.55
CHEMBL257453 Ki = 28.0 nM 7.55
CHEMBL272959 Ki = 44.5 nM 7.35
CHEMBL272772 Ki = 53.0 nM 7.28
CHEMBL402321 Ki = 61.0 nM 7.21
CHEMBL257451 Ki = 73.0 nM 7.14
CHEMBL272737 Ki = 78.0 nM 7.11
CHEMBL257240 Ki = 100.0 nM 7.00
CHEMBL442804 Ki = 160.0 nM 6.80
CHEMBL256458 Ki = 200.0 nM 6.70
CHEMBL409678 Ki = 260.0 nM 6.58
CHEMBL272116 Ki = 270.0 nM 6.57
CHEMBL257319 Ki = 370.0 nM 6.43
CHEMBL257242 Ki = 380.0 nM 6.42
CHEMBL257241 Ki = 420.0 nM 6.38
CHEMBL272976 Ki = 450.0 nM 6.35
CHEMBL272977 Ki = 560.0 nM 6.25
CHEMBL402730 Ki = 650.0 nM 6.19