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Assay Detail

CHEMBL1273257

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Binding
Inhibition of factor 10a
128
Total Activities
126
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Coagulation factor X (CHEMBL244)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Factor Xa inhibitors: next-generation antithrombotic agents.
Pinto DJ, Smallheer JM, Cheney DL, Knabb RM, Wexler RR.
J Med Chem (2010) 53 : 6243 -6274
PubMed 20503967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 87 8.62 10.89
IC50 41 8.28 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL37251 1 10.89
CHEMBL378093 1 10.52
CHEMBL471725 1 10.36
CHEMBL221906 1 10.36
CHEMBL260085 1 10.24
CHEMBL231779 APIXABAN 4.0 1 10.10
CHEMBL1270651 1 10.00
CHEMBL474678 1 10.00
CHEMBL73193 FIDEXABAN 2.0 1 10.00
CHEMBL512351 BETRIXABAN 4.0 1 9.92
CHEMBL414002 1 9.89
CHEMBL140072 1 9.82
CHEMBL176140 1 9.82
CHEMBL1229814 1 9.80
CHEMBL438647 1 9.77
CHEMBL222079 1 9.74
CHEMBL206335 RAZAXABAN 2.0 1 9.72
CHEMBL595475 1 9.70
CHEMBL402109 1 9.70
CHEMBL54237 1 9.49
CHEMBL476186 ERIBAXABAN 2.0 1 9.49
CHEMBL1269832 1 9.42
CHEMBL198362 RIVAROXABAN 4.0 2 9.40
CHEMBL233992 1 9.37
CHEMBL593461 1 9.30
CHEMBL46618 OTAMIXABAN 3.0 1 9.30
CHEMBL450578 1 9.29
CHEMBL1271368 1 9.26
CHEMBL1269025 EDOXABAN 4.0 1 9.25
CHEMBL1271369 1 9.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL37251 Ki = 0.013 nM 10.89
CHEMBL378093 Ki = 0.03 nM 10.52
CHEMBL221906 Ki = 0.044 nM 10.36
CHEMBL471725 Ki = 0.044 nM 10.36
CHEMBL260085 Ki = 0.057 nM 10.24
CHEMBL231779 APIXABAN Ki = 0.08 nM 10.10
CHEMBL73193 FIDEXABAN Ki = 0.1 nM 10.00
CHEMBL474678 IC50 = 0.1 nM 10.00
CHEMBL1270651 Ki = 0.1 nM 10.00
CHEMBL512351 BETRIXABAN Ki = 0.12 nM 9.92
CHEMBL414002 IC50 = 0.13 nM 9.89
CHEMBL176140 Ki = 0.15 nM 9.82
CHEMBL140072 Ki = 0.15 nM 9.82
CHEMBL1229814 IC50 = 0.16 nM 9.80
CHEMBL438647 Ki = 0.17 nM 9.77
CHEMBL222079 Ki = 0.18 nM 9.74
CHEMBL206335 RAZAXABAN Ki = 0.19 nM 9.72
CHEMBL595475 Ki = 0.2 nM 9.70
CHEMBL402109 Ki = 0.2 nM 9.70
CHEMBL54237 Ki = 0.32 nM 9.49
CHEMBL476186 ERIBAXABAN IC50 = 0.32 nM 9.49
CHEMBL1269832 IC50 = 0.38 nM 9.42
CHEMBL198362 RIVAROXABAN Ki = 0.4 nM 9.40
CHEMBL233992 Ki = 0.43 nM 9.37
CHEMBL593461 Ki = 0.5 nM 9.30
CHEMBL46618 OTAMIXABAN Ki = 0.5 nM 9.30
CHEMBL450578 Ki = 0.51 nM 9.29
CHEMBL1271368 Ki = 0.55 nM 9.26
CHEMBL1269025 EDOXABAN Ki = 0.56 nM 9.25
CHEMBL1271369 Ki = 0.6 nM 9.22
CHEMBL176243 Ki = 0.6 nM 9.22
CHEMBL398380 Ki = 0.67 nM 9.17
CHEMBL279486 Ki = 0.7 nM 9.15
CHEMBL1271056 Ki = 0.7 nM 9.15
CHEMBL198362 RIVAROXABAN IC50 = 0.7 nM 9.15
CHEMBL173650 Ki = 0.8 nM 9.10
CHEMBL1270358 IC50 = 0.83 nM 9.08
CHEMBL1271161 Ki = 0.9 nM 9.05
CHEMBL151939 Ki = 0.91 nM 9.04
CHEMBL1270158 Ki = 0.97 nM 9.01
CHEMBL182597 Ki = 1.0 nM 9.00
CHEMBL384526 Ki = 1.1 nM 8.96
CHEMBL423417 Ki = 1.1 nM 8.96
CHEMBL1269024 IC50 = 1.2 nM 8.92
CHEMBL20240 YM-60828 Ki = 1.3 nM 8.89
CHEMBL369086 Ki = 1.3 nM 8.89
CHEMBL279287 Ki = 1.5 nM 8.82
CHEMBL367953 Ki = 1.5 nM 8.82
CHEMBL463385 Ki = 1.7 nM 8.77
CHEMBL1095032 LETAXABAN Ki = 1.8 nM 8.74