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Assay Detail

CHEMBL816079

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Binding
Inhibitory activity against thrombin (IIa) was determined
ChEMBL ↗
95
Total Activities
95
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, parallel synthesis, and crystal structures of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.
Parlow JJ, Case BL, Dice TA, Fenton RL, Hayes MJ, Jones DE, Neumann WL, Wood RS, Lachance RM, Girard TJ, Nicholson NS, Clare M, Stegeman RA, Stevens AM, Stallings WC, Kurumbail RG, South MS.
J Med Chem (2003) 46 : 4050 -4062
PubMed 12954058 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 95 5.51 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL132855 — — 1 7.22
CHEMBL412136 — — 1 7.00
CHEMBL130443 — — 1 7.00
CHEMBL127554 — — 1 6.96
CHEMBL131190 — — 1 6.82
CHEMBL75084 — — 1 6.80
CHEMBL335484 — — 1 6.70
CHEMBL336144 — — 1 6.52
CHEMBL131326 — — 1 6.52
CHEMBL130100 — — 1 6.52
CHEMBL335406 — — 1 6.24
CHEMBL335187 — — 1 6.14
CHEMBL132151 — — 1 6.05
CHEMBL337678 — — 1 6.05
CHEMBL335491 — — 1 6.01
CHEMBL131056 — — 1 6.00
CHEMBL335076 — — 1 6.00
CHEMBL133125 — — 1 5.96
CHEMBL128284 — — 1 5.96
CHEMBL132051 — — 1 5.92
CHEMBL133404 — — 1 5.92
CHEMBL339692 — — 1 5.70
CHEMBL130897 — — 1 5.70
CHEMBL130812 — — 1 5.68
CHEMBL337278 — — 1 5.68
CHEMBL131473 — — 1 5.55
CHEMBL127553 — — 1 5.52
CHEMBL335755 — — 1 5.51
CHEMBL336977 — — 1 5.49
CHEMBL422079 — — 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL132855 — IC50 = 60.0 nM 7.22
CHEMBL412136 — IC50 = 100.0 nM 7.00
CHEMBL130443 — IC50 = 100.0 nM 7.00
CHEMBL127554 — IC50 = 110.0 nM 6.96
CHEMBL131190 — IC50 = 150.0 nM 6.82
CHEMBL75084 — IC50 = 160.0 nM 6.80
CHEMBL335484 — IC50 = 200.0 nM 6.70
CHEMBL336144 — IC50 = 300.0 nM 6.52
CHEMBL131326 — IC50 = 300.0 nM 6.52
CHEMBL130100 — IC50 = 300.0 nM 6.52
CHEMBL335406 — IC50 = 580.0 nM 6.24
CHEMBL335187 — IC50 = 720.0 nM 6.14
CHEMBL132151 — IC50 = 900.0 nM 6.05
CHEMBL337678 — IC50 = 890.0 nM 6.05
CHEMBL335491 — IC50 = 980.0 nM 6.01
CHEMBL131056 — IC50 = 1000.0 nM 6.00
CHEMBL335076 — IC50 = 1000.0 nM 6.00
CHEMBL133125 — IC50 = 1100.0 nM 5.96
CHEMBL128284 — IC50 = 1100.0 nM 5.96
CHEMBL132051 — IC50 = 1200.0 nM 5.92
CHEMBL133404 — IC50 = 1200.0 nM 5.92
CHEMBL339692 — IC50 = 2000.0 nM 5.70
CHEMBL130897 — IC50 = 2000.0 nM 5.70
CHEMBL130812 — IC50 = 2100.0 nM 5.68
CHEMBL337278 — IC50 = 2100.0 nM 5.68
CHEMBL131473 — IC50 = 2800.0 nM 5.55
CHEMBL127553 — IC50 = 3000.0 nM 5.52
CHEMBL335755 — IC50 = 3100.0 nM 5.51
CHEMBL336977 — IC50 = 3210.0 nM 5.49
CHEMBL422079 — IC50 = 3300.0 nM 5.48
CHEMBL131947 — IC50 = 3500.0 nM 5.46
CHEMBL130178 — IC50 = 4000.0 nM 5.40
CHEMBL130537 — IC50 = 4000.0 nM 5.40
CHEMBL130815 — IC50 = 4060.0 nM 5.39
CHEMBL133009 — IC50 = 4250.0 nM 5.37
CHEMBL338869 — IC50 = 4400.0 nM 5.36
CHEMBL131878 — IC50 = 4600.0 nM 5.34
CHEMBL131250 — IC50 = 5200.0 nM 5.28
CHEMBL131601 — IC50 = 5200.0 nM 5.28
CHEMBL340945 — IC50 = 6300.0 nM 5.20
CHEMBL444600 — IC50 = 6980.0 nM 5.16
CHEMBL338952 — IC50 = 7100.0 nM 5.15
CHEMBL133623 — IC50 = 7630.0 nM 5.12
CHEMBL130447 — IC50 = 8000.0 nM 5.10
CHEMBL130166 — IC50 = 8000.0 nM 5.10
CHEMBL341487 — IC50 = 8000.0 nM 5.10
CHEMBL338322 — IC50 = 8600.0 nM 5.07
CHEMBL436370 — IC50 = 8700.0 nM 5.06
CHEMBL423521 — IC50 = 10000.0 nM 5.00
CHEMBL130067 — IC50 = 10000.0 nM 5.00