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Assay Detail

CHEMBL4380985

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Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL ↗
58
Total Activities
28
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

C3a anaphylatoxin chemotactic receptor (CHEMBL4761) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity.
Rowley JA, Reid RC, Poon EKY, Wu KC, Lim J, Lohman RJ, Hamidon JK, Yau MK, Halili MA, Durek T, Iyer A, Fairlie DP.
J Med Chem (2020) 63 : 529 -541
PubMed 31910011 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 56 6.83 8.52
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4445758 — — 2 8.52
CHEMBL4559976 — — 2 8.40
CHEMBL4459830 — — 2 8.22
CHEMBL4470864 — — 3 8.20
CHEMBL4459627 — — 3 8.00
CHEMBL4558167 — — 2 7.52
CHEMBL4473192 — — 2 7.50
CHEMBL4559463 — — 2 7.40
CHEMBL4576800 — — 2 7.10
CHEMBL4455385 — — 2 7.05
CHEMBL4562412 — — 2 7.00
CHEMBL4472149 — — 2 7.00
CHEMBL4551058 — — 2 6.90
CHEMBL4472196 — — 2 6.90
CHEMBL4458380 — — 2 6.70
CHEMBL4592883 — — 2 6.30
CHEMBL4439578 — — 2 6.22
CHEMBL4470384 — — 2 6.10
CHEMBL389348 — — 2 5.89
CHEMBL4444281 — — 2 5.70
CHEMBL4530755 — — 2 5.64
CHEMBL4551118 — — 2 5.62
CHEMBL4572633 — — 2 5.40
CHEMBL4472490 — — 2 5.21
CHEMBL4519060 — — 2 -
CHEMBL4556174 — — 2 -
CHEMBL4521007 — — 2 -
CHEMBL4439168 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4445758 — IC50 = 3.0 nM 8.52
CHEMBL4445758 — IC50 = 3.162 nM 8.50
CHEMBL4559976 — IC50 = 4.0 nM 8.40
CHEMBL4559976 — IC50 = 3.981 nM 8.40
CHEMBL4459830 — IC50 = 6.0 nM 8.22
CHEMBL4459830 — IC50 = 6.31 nM 8.20
CHEMBL4470864 — IC50 = 6.31 nM 8.20
CHEMBL4470864 — IC50 = 7.0 nM 8.15
CHEMBL4459627 — IC50 = 10.0 nM 8.00
CHEMBL4459627 — IC50 = 10.0 nM 8.00
CHEMBL4558167 — IC50 = 30.0 nM 7.52
CHEMBL4558167 — IC50 = 31.62 nM 7.50
CHEMBL4473192 — IC50 = 31.62 nM 7.50
CHEMBL4473192 — IC50 = 35.0 nM 7.46
CHEMBL4559463 — IC50 = 39.81 nM 7.40
CHEMBL4559463 — IC50 = 40.0 nM 7.40
CHEMBL4576800 — IC50 = 79.43 nM 7.10
CHEMBL4576800 — IC50 = 85.0 nM 7.07
CHEMBL4455385 — IC50 = 90.0 nM 7.05
CHEMBL4472149 — IC50 = 100.0 nM 7.00
CHEMBL4455385 — IC50 = 100.0 nM 7.00
CHEMBL4562412 — IC50 = 100.0 nM 7.00
CHEMBL4562412 — IC50 = 100.0 nM 7.00
CHEMBL4472149 — IC50 = 100.0 nM 7.00
CHEMBL4472196 — IC50 = 125.89 nM 6.90
CHEMBL4551058 — IC50 = 125.89 nM 6.90
CHEMBL4551058 — IC50 = 140.0 nM 6.85
CHEMBL4472196 — IC50 = 140.0 nM 6.85
CHEMBL4458380 — IC50 = 199.53 nM 6.70
CHEMBL4458380 — IC50 = 200.0 nM 6.70
CHEMBL4592883 — IC50 = 501.19 nM 6.30
CHEMBL4592883 — IC50 = 510.0 nM 6.29
CHEMBL4439578 — IC50 = 600.0 nM 6.22
CHEMBL4439578 — IC50 = 630.96 nM 6.20
CHEMBL4470384 — IC50 = 794.33 nM 6.10
CHEMBL4470384 — IC50 = 790.0 nM 6.10
CHEMBL389348 — IC50 = 1300.0 nM 5.89
CHEMBL4444281 — IC50 = 1995.26 nM 5.70
CHEMBL4444281 — IC50 = 2000.0 nM 5.70
CHEMBL4530755 — IC50 = 2300.0 nM 5.64
CHEMBL4551118 — IC50 = 2400.0 nM 5.62
CHEMBL4530755 — IC50 = 2511.89 nM 5.60
CHEMBL4551118 — IC50 = 2511.89 nM 5.60
CHEMBL389348 — IC50 = 3981.07 nM 5.40
CHEMBL4572633 — IC50 = 3981.07 nM 5.40
CHEMBL4572633 — IC50 = 4400.0 nM 5.36
CHEMBL4472490 — IC50 = 6100.0 nM 5.21
CHEMBL4472490 — IC50 = 6309.57 nM 5.20
CHEMBL4521007 — IC50 > 10000.0 nM -
CHEMBL4556174 — IC50 > 100000.0 nM -