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Assay Detail

CHEMBL865639

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

Binding
Inhibition of C1S
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Complement C1s subcomponent (CHEMBL3913)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.
Subasinghe NL, Travins JM, Ali F, Huang H, Ballentine SK, Marugán JJ, Khalil E, Hufnagel HR, Bone RF, DesJarlais RL, Crysler CS, Ninan N, Cummings MD, Molloy CJ, Tomczuk BE.
Bioorg Med Chem Lett (2006) 16 : 2200 -2204
PubMed 16460935 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 6.58 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL205904 1 8.00
CHEMBL377090 1 7.70
CHEMBL438807 1 7.52
CHEMBL377281 1 7.52
CHEMBL382350 1 7.40
CHEMBL206020 1 7.30
CHEMBL381771 1 7.16
CHEMBL382443 1 7.00
CHEMBL205385 1 7.00
CHEMBL426490 1 6.80
CHEMBL205804 1 6.77
CHEMBL381097 1 6.77
CHEMBL205342 1 6.75
CHEMBL380315 1 6.70
CHEMBL377934 1 6.68
CHEMBL438267 1 6.62
CHEMBL204679 1 6.51
CHEMBL205578 1 6.48
CHEMBL205657 1 6.48
CHEMBL205354 1 6.42
CHEMBL379523 1 6.40
CHEMBL380325 1 6.40
CHEMBL205698 1 6.40
CHEMBL204889 1 6.40
CHEMBL380318 1 6.39
CHEMBL204936 1 6.38
CHEMBL382447 1 6.24
CHEMBL205489 1 6.12
CHEMBL382626 1 5.75
CHEMBL380146 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL205904 Ki = 10.0 nM 8.00
CHEMBL377090 Ki = 20.0 nM 7.70
CHEMBL438807 Ki = 30.0 nM 7.52
CHEMBL377281 Ki = 30.0 nM 7.52
CHEMBL382350 Ki = 40.0 nM 7.40
CHEMBL206020 Ki = 50.0 nM 7.30
CHEMBL381771 Ki = 70.0 nM 7.16
CHEMBL382443 Ki = 100.0 nM 7.00
CHEMBL205385 Ki = 100.0 nM 7.00
CHEMBL426490 Ki = 160.0 nM 6.80
CHEMBL205804 Ki = 170.0 nM 6.77
CHEMBL381097 Ki = 170.0 nM 6.77
CHEMBL205342 Ki = 180.0 nM 6.75
CHEMBL380315 Ki = 200.0 nM 6.70
CHEMBL377934 Ki = 210.0 nM 6.68
CHEMBL438267 Ki = 240.0 nM 6.62
CHEMBL204679 Ki = 310.0 nM 6.51
CHEMBL205578 Ki = 330.0 nM 6.48
CHEMBL205657 Ki = 330.0 nM 6.48
CHEMBL205354 Ki = 380.0 nM 6.42
CHEMBL379523 Ki = 400.0 nM 6.40
CHEMBL380325 Ki = 400.0 nM 6.40
CHEMBL205698 Ki = 400.0 nM 6.40
CHEMBL204889 Ki = 400.0 nM 6.40
CHEMBL380318 Ki = 410.0 nM 6.39
CHEMBL204936 Ki = 420.0 nM 6.38
CHEMBL382447 Ki = 580.0 nM 6.24
CHEMBL205489 Ki = 750.0 nM 6.12
CHEMBL382626 Ki = 1790.0 nM 5.75
CHEMBL380146 Ki = 1880.0 nM 5.73
CHEMBL383619 Ki = 2000.0 nM 5.70
CHEMBL383083 Ki = 2240.0 nM 5.65
CHEMBL208449 Ki = 2290.0 nM 5.64
CHEMBL377438 Ki = 11000.0 nM 4.96