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Assay Detail

CHEMBL3734190

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

Functional
Antagonist activity against human P2X2/3 receptor expressed in HEK293/1321N1 cells assessed as inhibition of alpha,beta-meATP/ATP-induced calcium influx by Fluo-4 dye based FLIPR assay
93
Total Activities
93
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

P2X2/P2X3 heterotrimeric receptor (CHEMBL3831281)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

2-cyanophenyl fused heterocyclic compounds, and compositions and uses thereof
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 93 6.63 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3731399 1 7.92
CHEMBL3732843 1 7.72
CHEMBL3728821 1 7.72
CHEMBL3730913 1 7.70
CHEMBL3731410 1 7.62
CHEMBL3729264 1 7.60
CHEMBL3732909 1 7.57
CHEMBL3727382 1 7.55
CHEMBL3732309 1 7.52
CHEMBL3731936 1 7.51
CHEMBL3731366 1 7.48
CHEMBL3731764 1 7.48
CHEMBL3728949 1 7.38
CHEMBL3733189 1 7.38
CHEMBL3732959 1 7.37
CHEMBL3733173 1 7.35
CHEMBL3730584 1 7.35
CHEMBL3731980 1 7.35
CHEMBL3728301 1 7.30
CHEMBL3732382 1 7.26
CHEMBL3729278 1 7.23
CHEMBL3730477 1 7.21
CHEMBL3730649 1 7.21
CHEMBL3733102 1 7.20
CHEMBL3729724 1 7.17
CHEMBL3731231 1 7.15
CHEMBL3731419 1 7.09
CHEMBL3730174 1 7.09
CHEMBL3730205 1 7.04
CHEMBL3729891 1 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3731399 IC50 = 12.0 nM 7.92
CHEMBL3732843 IC50 = 19.0 nM 7.72
CHEMBL3728821 IC50 = 19.0 nM 7.72
CHEMBL3730913 IC50 = 20.0 nM 7.70
CHEMBL3731410 IC50 = 24.0 nM 7.62
CHEMBL3729264 IC50 = 25.0 nM 7.60
CHEMBL3732909 IC50 = 27.0 nM 7.57
CHEMBL3727382 IC50 = 28.0 nM 7.55
CHEMBL3732309 IC50 = 30.0 nM 7.52
CHEMBL3731936 IC50 = 31.0 nM 7.51
CHEMBL3731366 IC50 = 33.0 nM 7.48
CHEMBL3731764 IC50 = 33.0 nM 7.48
CHEMBL3728949 IC50 = 42.0 nM 7.38
CHEMBL3733189 IC50 = 42.0 nM 7.38
CHEMBL3732959 IC50 = 43.0 nM 7.37
CHEMBL3733173 IC50 = 45.0 nM 7.35
CHEMBL3731980 IC50 = 45.0 nM 7.35
CHEMBL3730584 IC50 = 45.0 nM 7.35
CHEMBL3728301 IC50 = 50.0 nM 7.30
CHEMBL3732382 IC50 = 55.0 nM 7.26
CHEMBL3729278 IC50 = 59.0 nM 7.23
CHEMBL3730477 IC50 = 61.0 nM 7.21
CHEMBL3730649 IC50 = 62.0 nM 7.21
CHEMBL3733102 IC50 = 63.0 nM 7.20
CHEMBL3729724 IC50 = 67.0 nM 7.17
CHEMBL3731231 IC50 = 71.0 nM 7.15
CHEMBL3730174 IC50 = 82.0 nM 7.09
CHEMBL3731419 IC50 = 82.0 nM 7.09
CHEMBL3730205 IC50 = 92.0 nM 7.04
CHEMBL3729891 IC50 = 92.0 nM 7.04
CHEMBL3730868 IC50 = 92.0 nM 7.04
CHEMBL3729489 IC50 = 105.0 nM 6.98
CHEMBL3732409 IC50 = 120.0 nM 6.92
CHEMBL3729478 IC50 = 124.0 nM 6.91
CHEMBL3731305 IC50 = 127.0 nM 6.90
CHEMBL3731744 IC50 = 125.0 nM 6.90
CHEMBL3732414 IC50 = 130.0 nM 6.89
CHEMBL3732154 IC50 = 136.0 nM 6.87
CHEMBL3733209 IC50 = 152.0 nM 6.82
CHEMBL3732768 IC50 = 164.0 nM 6.79
CHEMBL3727897 IC50 = 169.0 nM 6.77
CHEMBL3729611 IC50 = 174.0 nM 6.76
CHEMBL3727954 IC50 = 180.0 nM 6.75
CHEMBL3732185 IC50 = 200.0 nM 6.70
CHEMBL3728501 IC50 = 224.0 nM 6.65
CHEMBL3729987 IC50 = 225.0 nM 6.65
CHEMBL3729871 IC50 = 241.0 nM 6.62
CHEMBL3732208 IC50 = 246.0 nM 6.61
CHEMBL3728453 IC50 = 263.0 nM 6.58
CHEMBL3732421 IC50 = 273.0 nM 6.56