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Assay Detail

CHEMBL3854654

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

Binding
Inhibition of full-length human TF/recombinant human factor 7a assessed as decrease in conversion of factor 10 to factor 10a by measuring S2765 hydrolysis after 15 mins
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Coagulation factor VII/tissue factor (CHEMBL2095194)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.
Zhang X, Glunz PW, Johnson JA, Jiang W, Jacutin-Porte S, Ladziata V, Zou Y, Phillips MS, Wurtz NR, Parkhurst B, Rendina AR, Harper TM, Cheney DL, Luettgen JM, Wong PC, Seiffert D, Wexler RR, Priestley ES.
J Med Chem (2016) 59 : 7125 -7137
PubMed 27455395 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.84 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3891120 1 9.80
CHEMBL3901391 1 9.64
CHEMBL3978562 1 9.55
CHEMBL3902498 1 9.37
CHEMBL3917434 1 9.24
CHEMBL3980787 1 9.21
CHEMBL3909009 1 9.00
CHEMBL3951940 1 8.66
CHEMBL3930523 1 8.60
CHEMBL3935309 1 8.26
CHEMBL3942944 1 8.06
CHEMBL3926417 1 7.82
CHEMBL3907376 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3891120 Ki = 0.16 nM 9.80
CHEMBL3901391 Ki = 0.23 nM 9.64
CHEMBL3978562 Ki = 0.28 nM 9.55
CHEMBL3902498 Ki = 0.43 nM 9.37
CHEMBL3917434 Ki = 0.57 nM 9.24
CHEMBL3980787 Ki = 0.61 nM 9.21
CHEMBL3909009 Ki = 1.0 nM 9.00
CHEMBL3951940 Ki = 2.2 nM 8.66
CHEMBL3930523 Ki = 2.5 nM 8.60
CHEMBL3935309 Ki = 5.5 nM 8.26
CHEMBL3942944 Ki = 8.7 nM 8.06
CHEMBL3926417 Ki = 15.0 nM 7.82
CHEMBL3907376 Ki = 20.0 nM 7.70