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Assay Detail

CHEMBL3259187

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

Binding
Competitive reversible inhibition of bovine trypsin using alpha-N-benzoyl-DL-arginine-p-nitroanilide hydrochloride as substrate after 15 to 30 mins by Michaelis-Menten plot analysis
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Diarylamidine derivatives with one or both of the aryl moieties consisting of an indole or indole-like ring. Inhibitors of arginine-specific esteroproteases.
Tidwell RR, Geratz JD, Dann O, Volz G, Zeh D, Loewe H.
J Med Chem (1978) 21 : 613 -623
PubMed 671460 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 62 5.13 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99951 1 7.77
CHEMBL101672 1 5.84
CHEMBL168077 1 5.67
CHEMBL279962 1 5.65
CHEMBL167983 1 5.60
CHEMBL167255 1 5.59
CHEMBL3251534 1 5.56
CHEMBL102148 1 5.53
CHEMBL3251529 1 5.49
CHEMBL165312 1 5.49
CHEMBL167845 1 5.48
CHEMBL167801 1 5.47
CHEMBL289577 1 5.42
CHEMBL352923 1 5.41
CHEMBL103649 1 5.40
CHEMBL3251186 1 5.38
CHEMBL3251191 1 5.38
CHEMBL352553 1 5.38
CHEMBL356487 1 5.33
CHEMBL3251527 1 5.33
CHEMBL167762 1 5.33
CHEMBL52393 1 5.31
CHEMBL48217 DAPI 1 5.28
CHEMBL164947 1 5.24
CHEMBL297809 1 5.23
CHEMBL101261 1 5.22
CHEMBL167761 1 5.21
CHEMBL3251528 1 5.19
CHEMBL3251192 1 5.18
CHEMBL166236 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99951 Ki = 17.0 nM 7.77
CHEMBL101672 Ki = 1440.0 nM 5.84
CHEMBL168077 Ki = 2130.0 nM 5.67
CHEMBL279962 Ki = 2240.0 nM 5.65
CHEMBL167983 Ki = 2490.0 nM 5.60
CHEMBL167255 Ki = 2590.0 nM 5.59
CHEMBL3251534 Ki = 2750.0 nM 5.56
CHEMBL102148 Ki = 2960.0 nM 5.53
CHEMBL3251529 Ki = 3230.0 nM 5.49
CHEMBL165312 Ki = 3250.0 nM 5.49
CHEMBL167845 Ki = 3320.0 nM 5.48
CHEMBL167801 Ki = 3390.0 nM 5.47
CHEMBL289577 Ki = 3790.0 nM 5.42
CHEMBL352923 Ki = 3940.0 nM 5.41
CHEMBL103649 Ki = 4010.0 nM 5.40
CHEMBL3251186 Ki = 4160.0 nM 5.38
CHEMBL352553 Ki = 4170.0 nM 5.38
CHEMBL3251191 Ki = 4190.0 nM 5.38
CHEMBL356487 Ki = 4680.0 nM 5.33
CHEMBL3251527 Ki = 4670.0 nM 5.33
CHEMBL167762 Ki = 4730.0 nM 5.33
CHEMBL52393 Ki = 4930.0 nM 5.31
CHEMBL48217 DAPI Ki = 5310.0 nM 5.28
CHEMBL164947 Ki = 5800.0 nM 5.24
CHEMBL297809 Ki = 5880.0 nM 5.23
CHEMBL101261 Ki = 5980.0 nM 5.22
CHEMBL167761 Ki = 6170.0 nM 5.21
CHEMBL3251528 Ki = 6520.0 nM 5.19
CHEMBL3251192 Ki = 6570.0 nM 5.18
CHEMBL166236 Ki = 6670.0 nM 5.18
CHEMBL3251535 Ki = 7110.0 nM 5.15
CHEMBL354342 Ki = 7270.0 nM 5.14
CHEMBL500330 Ki = 9300.0 nM 5.03
CHEMBL3244501 Ki = 9320.0 nM 5.03
CHEMBL297403 Ki = 9460.0 nM 5.02
CHEMBL1233459 Ki = 9800.0 nM 5.01
CHEMBL3251538 Ki = 10800.0 nM 4.97
CHEMBL388768 Ki = 11100.0 nM 4.96
CHEMBL3251190 Ki = 11600.0 nM 4.94
CHEMBL3251187 Ki = 13100.0 nM 4.88
CHEMBL1688696 Ki = 14600.0 nM 4.84
CHEMBL164489 Ki = 15600.0 nM 4.81
CHEMBL3251537 Ki = 16200.0 nM 4.79
CHEMBL417907 Ki = 17000.0 nM 4.77
CHEMBL563834 Ki = 17100.0 nM 4.77
CHEMBL3251536 Ki = 18000.0 nM 4.75
CHEMBL3251185 Ki = 19400.0 nM 4.71
CHEMBL3251189 Ki = 24400.0 nM 4.61
CHEMBL3251188 Ki = 27200.0 nM 4.57
CHEMBL145656 Ki = 27800.0 nM 4.56