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Assay Detail

CHEMBL662444

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Binding
Binding affinity against human coagulation factor X
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa.
Pinto DJ, Orwat MJ, Wang S, Fevig JM, Quan ML, Amparo E, Cacciola J, Rossi KA, Alexander RS, Smallwood AM, Luettgen JM, Liang L, Aungst BJ, Wright MR, Knabb RM, Wong PC, Wexler RR, Lam PY.
J Med Chem (2001) 44 : 566 -578
PubMed 11170646 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 8.70 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL152859 1 11.00
CHEMBL152854 1 10.89
CHEMBL347846 1 10.82
CHEMBL422688 1 10.70
CHEMBL154512 1 10.40
CHEMBL421808 1 10.39
CHEMBL347931 1 10.22
CHEMBL153611 1 9.82
CHEMBL356016 1 9.80
CHEMBL346834 1 9.54
CHEMBL152276 1 9.34
CHEMBL152274 1 9.10
CHEMBL444074 1 8.89
CHEMBL134736 1 8.57
CHEMBL358834 1 7.96
CHEMBL559015 1 6.82
CHEMBL154680 1 6.44
CHEMBL153946 1 6.42
CHEMBL422351 1 6.32
CHEMBL156775 1 6.05
CHEMBL154504 1 6.04
CHEMBL154572 1 5.80
CHEMBL346686 1 -
CHEMBL154322 1 -
CHEMBL358835 1 -
CHEMBL152281 1 -
CHEMBL347307 1 -
CHEMBL346857 1 -
CHEMBL440733 1 -
CHEMBL154238 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL152859 Ki = 0.01 nM 11.00
CHEMBL152854 Ki = 0.013 nM 10.89
CHEMBL347846 Ki = 0.015 nM 10.82
CHEMBL422688 Ki = 0.02 nM 10.70
CHEMBL154512 Ki = 0.04 nM 10.40
CHEMBL421808 Ki = 0.041 nM 10.39
CHEMBL347931 Ki = 0.06 nM 10.22
CHEMBL153611 Ki = 0.15 nM 9.82
CHEMBL356016 Ki = 0.16 nM 9.80
CHEMBL346834 Ki = 0.29 nM 9.54
CHEMBL152276 Ki = 0.46 nM 9.34
CHEMBL152274 Ki = 0.8 nM 9.10
CHEMBL444074 Ki = 1.3 nM 8.89
CHEMBL134736 Ki = 2.7 nM 8.57
CHEMBL358834 Ki = 11.0 nM 7.96
CHEMBL559015 Ki = 150.0 nM 6.82
CHEMBL154680 Ki = 360.0 nM 6.44
CHEMBL153946 Ki = 380.0 nM 6.42
CHEMBL422351 Ki = 480.0 nM 6.32
CHEMBL156775 Ki = 890.0 nM 6.05
CHEMBL154504 Ki = 910.0 nM 6.04
CHEMBL154572 Ki = 1600.0 nM 5.80
CHEMBL346686 Ki = 0.009 nM -
CHEMBL154322 Ki = 0.007 nM -
CHEMBL358835 Ki < 5.0 nM -
CHEMBL152281 Ki < 0.005 nM -
CHEMBL347307 Ki = 0.005 nM -
CHEMBL346857 Ki = 0.001 nM -
CHEMBL440733 Ki = 0.008 nM -
CHEMBL154238 Ki = 0.008 nM -
CHEMBL359132 Ki = 0.009 nM -