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Assay Detail

CHEMBL813660

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Binding
Inhibition against human thrombin
32
Total Activities
32
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

Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors.
Duncia JV, Santella JB, Higley CA, VanAtten MK, Weber PC, Alexander RS, Kettner CA, Pruitt JR, Liauw AY, Quan ML, Knabb RM, Wexler RR.
Bioorg Med Chem Lett (1998) 8 : 775 -780
PubMed 9871540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 7.56 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423259 1 9.52
CHEMBL2373405 1 9.10
CHEMBL317682 1 8.77
CHEMBL2373403 1 8.74
CHEMBL2373408 1 8.59
CHEMBL2375178 1 8.46
CHEMBL2373351 1 8.34
CHEMBL2373367 1 8.26
CHEMBL2373349 1 8.07
CHEMBL2373344 1 8.06
CHEMBL2373397 1 7.96
CHEMBL2373342 1 7.51
CHEMBL2373440 1 7.48
CHEMBL2373399 1 7.48
CHEMBL2373559 1 7.48
CHEMBL2373558 1 7.44
CHEMBL2373401 1 7.39
CHEMBL2373475 1 7.33
CHEMBL2373350 1 7.19
CHEMBL2373402 1 7.14
CHEMBL2373341 1 7.08
CHEMBL2373555 1 7.07
CHEMBL2373347 1 7.07
CHEMBL2373348 1 6.82
CHEMBL2373345 1 6.82
CHEMBL2373346 1 6.80
CHEMBL2373343 1 6.76
CHEMBL2373302 1 6.68
CHEMBL2373400 1 6.64
CHEMBL2373352 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423259 Ki = 0.3 nM 9.52
CHEMBL2373405 Ki = 0.8 nM 9.10
CHEMBL317682 Ki = 1.71 nM 8.77
CHEMBL2373403 Ki = 1.8 nM 8.74
CHEMBL2373408 Ki = 2.6 nM 8.59
CHEMBL2375178 Ki = 3.5 nM 8.46
CHEMBL2373351 Ki = 4.6 nM 8.34
CHEMBL2373367 Ki = 5.5 nM 8.26
CHEMBL2373349 Ki = 8.6 nM 8.07
CHEMBL2373344 Ki = 8.7 nM 8.06
CHEMBL2373397 Ki = 11.0 nM 7.96
CHEMBL2373342 Ki = 31.0 nM 7.51
CHEMBL2373440 Ki = 33.0 nM 7.48
CHEMBL2373399 Ki = 33.0 nM 7.48
CHEMBL2373559 Ki = 33.0 nM 7.48
CHEMBL2373558 Ki = 36.0 nM 7.44
CHEMBL2373401 Ki = 41.0 nM 7.39
CHEMBL2373475 Ki = 47.0 nM 7.33
CHEMBL2373350 Ki = 65.0 nM 7.19
CHEMBL2373402 Ki = 73.0 nM 7.14
CHEMBL2373341 Ki = 84.0 nM 7.08
CHEMBL2373555 Ki = 85.0 nM 7.07
CHEMBL2373347 Ki = 85.0 nM 7.07
CHEMBL2373348 Ki = 150.0 nM 6.82
CHEMBL2373345 Ki = 150.0 nM 6.82
CHEMBL2373346 Ki = 160.0 nM 6.80
CHEMBL2373343 Ki = 173.0 nM 6.76
CHEMBL2373302 Ki = 210.0 nM 6.68
CHEMBL2373400 Ki = 230.0 nM 6.64
CHEMBL2373352 Ki = 350.0 nM 6.46
CHEMBL2373404 Ki = 1700.0 nM 5.77
CHEMBL2373519 Ki > 42.0 nM -