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Assay Detail

CHEMBL5217731

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Binding
Inhibition of human complement factor D using Z-L-Lys-SBzl hydrochloride as substrate preincubated for 15 mins followed by substrate addition and measured by colorimetric method based esterolytic assay
ChEMBL ↗
56
Total Activities
55
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Complement factor D (CHEMBL2176771) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Scaffold hopping via ring opening enables identification of acyclic compounds as new complement Factor D inhibitors.
Zhang W, Wu M, Vadlakonda S, Juarez L, Cheng X, Muppa S, Chintareddy V, Vogeti L, Kellogg-Yelder D, Williams J, Polach K, Chen X, Raman K, Babu YS, Kotian P.
Bioorg Med Chem (2022) 74 : 117034 -117034
PubMed 36272185 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 55 6.29 8.22
Ki 1 7.73 7.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3683753 — — 1 8.22
CHEMBL5220885 — — 2 7.73
CHEMBL5219696 — — 1 7.57
CHEMBL5220461 — — 1 7.55
CHEMBL5219562 — — 1 7.52
CHEMBL3678914 — — 1 7.52
CHEMBL5218975 — — 1 7.47
CHEMBL5220104 — — 1 7.47
CHEMBL5220699 — — 1 7.27
CHEMBL5218654 — — 1 7.17
CHEMBL5220812 — — 1 7.11
CHEMBL5220843 — — 1 7.08
CHEMBL5220585 — — 1 7.06
CHEMBL5219286 — — 1 7.05
CHEMBL5219765 — — 1 7.05
CHEMBL5219487 — — 1 7.05
CHEMBL5220245 — — 1 7.00
CHEMBL5219431 — — 1 7.00
CHEMBL5220535 — — 1 7.00
CHEMBL5218910 — — 1 6.92
CHEMBL5218983 — — 1 6.92
CHEMBL5219583 — — 1 6.89
CHEMBL5219632 — — 1 6.80
CHEMBL5219728 — — 1 6.80
CHEMBL5220542 — — 1 6.72
CHEMBL5219944 — — 1 6.64
CHEMBL5219460 — — 1 6.39
CHEMBL5219202 — — 1 6.28
CHEMBL5220503 — — 1 6.22
CHEMBL5220306 — — 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3683753 — IC50 = 6.0 nM 8.22
CHEMBL5220885 — Ki = 18.5 nM 7.73
CHEMBL5219696 — IC50 = 27.0 nM 7.57
CHEMBL5220461 — IC50 = 28.0 nM 7.55
CHEMBL3678914 — IC50 = 30.0 nM 7.52
CHEMBL5219562 — IC50 = 30.0 nM 7.52
CHEMBL5220104 — IC50 = 34.0 nM 7.47
CHEMBL5218975 — IC50 = 34.0 nM 7.47
CHEMBL5220885 — IC50 = 37.0 nM 7.43
CHEMBL5220699 — IC50 = 54.0 nM 7.27
CHEMBL5218654 — IC50 = 67.0 nM 7.17
CHEMBL5220812 — IC50 = 77.0 nM 7.11
CHEMBL5220843 — IC50 = 84.0 nM 7.08
CHEMBL5220585 — IC50 = 87.0 nM 7.06
CHEMBL5219487 — IC50 = 89.0 nM 7.05
CHEMBL5219765 — IC50 = 90.0 nM 7.05
CHEMBL5219286 — IC50 = 89.0 nM 7.05
CHEMBL5220245 — IC50 = 100.0 nM 7.00
CHEMBL5220535 — IC50 = 100.0 nM 7.00
CHEMBL5219431 — IC50 = 100.0 nM 7.00
CHEMBL5218983 — IC50 = 120.0 nM 6.92
CHEMBL5218910 — IC50 = 120.0 nM 6.92
CHEMBL5219583 — IC50 = 130.0 nM 6.89
CHEMBL5219728 — IC50 = 160.0 nM 6.80
CHEMBL5219632 — IC50 = 160.0 nM 6.80
CHEMBL5220542 — IC50 = 190.0 nM 6.72
CHEMBL5219944 — IC50 = 230.0 nM 6.64
CHEMBL5219460 — IC50 = 410.0 nM 6.39
CHEMBL5219202 — IC50 = 520.0 nM 6.28
CHEMBL5220503 — IC50 = 600.0 nM 6.22
CHEMBL5220306 — IC50 = 650.0 nM 6.19
CHEMBL5220187 — IC50 = 690.0 nM 6.16
CHEMBL5218658 — IC50 = 880.0 nM 6.06
CHEMBL5219376 — IC50 = 900.0 nM 6.05
CHEMBL5220172 — IC50 = 1100.0 nM 5.96
CHEMBL5219797 — IC50 = 1300.0 nM 5.89
CHEMBL5220086 — IC50 = 1500.0 nM 5.82
CHEMBL5218912 — IC50 = 1900.0 nM 5.72
CHEMBL5220656 — IC50 = 3000.0 nM 5.52
CHEMBL5218908 — IC50 = 3400.0 nM 5.47
CHEMBL5220564 — IC50 = 4200.0 nM 5.38
CHEMBL5219504 — IC50 = 5300.0 nM 5.28
CHEMBL5219044 — IC50 = 9500.0 nM 5.02
CHEMBL5220368 — IC50 = 13000.0 nM 4.89
CHEMBL4076148 — IC50 = 14000.0 nM 4.85
CHEMBL5221126 — IC50 = 17000.0 nM 4.77
CHEMBL5221059 — IC50 = 23000.0 nM 4.64
CHEMBL5218913 — IC50 = 26000.0 nM 4.58
CHEMBL5220109 — IC50 = 35000.0 nM 4.46
CHEMBL5221048 — IC50 = 40000.0 nM 4.40