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Assay Detail

CHEMBL889318

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Binding
Inhibition of human F2a
ChEMBL ↗
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Prothrombin (CHEMBL204) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors.
Ye B, Arnaiz DO, Chou YL, Griedel BD, Karanjawala R, Lee W, Morrissey MM, Sacchi KL, Sakata ST, Shaw KJ, Wu SC, Zhao Z, Adler M, Cheeseman S, Dole WP, Ewing J, Fitch R, Lentz D, Liang A, Light D, Morser J, Post J, Rumennik G, Subramanyam B, Sullivan ME, Vergona R, Walters J, Wang YX, White KA, Whitlow M, Kochanny MJ.
J Med Chem (2007) 50 : 2967 -2980
PubMed 17536795 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 54 6.10 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL226669 — — 1 7.22
CHEMBL173994 — — 1 7.05
CHEMBL226668 — — 1 7.05
CHEMBL449702 — — 1 7.00
CHEMBL227360 — — 1 6.85
CHEMBL387856 — — 1 6.80
CHEMBL441880 — — 1 6.72
CHEMBL376791 — — 1 6.52
CHEMBL227307 — — 1 6.47
CHEMBL227308 — — 1 6.47
CHEMBL389638 — — 1 6.47
CHEMBL227359 — — 1 6.44
CHEMBL226615 — — 1 6.39
CHEMBL226827 — — 1 6.36
CHEMBL226931 — — 1 6.35
CHEMBL226564 — — 1 6.33
CHEMBL226826 — — 1 6.29
CHEMBL226616 — — 1 6.24
CHEMBL437546 — — 1 6.20
CHEMBL390055 — — 1 6.20
CHEMBL227171 — — 1 6.17
CHEMBL227196 — — 1 6.11
CHEMBL227121 — — 1 6.08
CHEMBL389210 — — 1 6.07
CHEMBL226825 — — 1 6.04
CHEMBL387857 — — 1 6.01
CHEMBL427421 — — 1 6.00
CHEMBL226721 — — 1 5.96
CHEMBL376790 — — 1 5.96
CHEMBL227249 — — 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL226669 — Ki = 60.0 nM 7.22
CHEMBL173994 — Ki = 90.0 nM 7.05
CHEMBL226668 — Ki = 90.0 nM 7.05
CHEMBL449702 — Ki = 100.0 nM 7.00
CHEMBL227360 — Ki = 140.0 nM 6.85
CHEMBL387856 — Ki = 160.0 nM 6.80
CHEMBL441880 — Ki = 190.0 nM 6.72
CHEMBL376791 — Ki = 300.0 nM 6.52
CHEMBL227307 — Ki = 340.0 nM 6.47
CHEMBL227308 — Ki = 340.0 nM 6.47
CHEMBL389638 — Ki = 340.0 nM 6.47
CHEMBL227359 — Ki = 360.0 nM 6.44
CHEMBL226615 — Ki = 410.0 nM 6.39
CHEMBL226827 — Ki = 440.0 nM 6.36
CHEMBL226931 — Ki = 450.0 nM 6.35
CHEMBL226564 — Ki = 470.0 nM 6.33
CHEMBL226826 — Ki = 510.0 nM 6.29
CHEMBL226616 — Ki = 580.0 nM 6.24
CHEMBL437546 — Ki = 630.0 nM 6.20
CHEMBL390055 — Ki = 630.0 nM 6.20
CHEMBL227171 — Ki = 680.0 nM 6.17
CHEMBL227196 — Ki = 770.0 nM 6.11
CHEMBL227121 — Ki = 840.0 nM 6.08
CHEMBL389210 — Ki = 860.0 nM 6.07
CHEMBL226825 — Ki = 920.0 nM 6.04
CHEMBL387857 — Ki = 970.0 nM 6.01
CHEMBL427421 — Ki = 990.0 nM 6.00
CHEMBL226721 — Ki = 1100.0 nM 5.96
CHEMBL376790 — Ki = 1100.0 nM 5.96
CHEMBL227249 — Ki = 1100.0 nM 5.96
CHEMBL226879 — Ki = 1100.0 nM 5.96
CHEMBL387656 — Ki = 1200.0 nM 5.92
CHEMBL227250 — Ki = 1200.0 nM 5.92
CHEMBL227172 — Ki = 1300.0 nM 5.89
CHEMBL227197 — Ki = 1400.0 nM 5.85
CHEMBL375264 — Ki = 1400.0 nM 5.85
CHEMBL227195 — Ki = 1400.0 nM 5.85
CHEMBL227146 — Ki = 1500.0 nM 5.82
CHEMBL226722 — Ki = 1500.0 nM 5.82
CHEMBL227221 — Ki = 1500.0 nM 5.82
CHEMBL375263 — Ki = 1700.0 nM 5.77
CHEMBL427276 — Ki = 1700.0 nM 5.77
CHEMBL425311 — Ki = 2000.0 nM 5.70
CHEMBL227248 — Ki = 2100.0 nM 5.68
CHEMBL226775 — Ki = 2200.0 nM 5.66
CHEMBL227223 — Ki = 2600.0 nM 5.58
CHEMBL449703 — Ki = 2600.0 nM 5.58
CHEMBL450012 — Ki = 3300.0 nM 5.48
CHEMBL226776 — Ki = 3300.0 nM 5.48
CHEMBL390969 — Ki = 3500.0 nM 5.46