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Assay Detail

CHEMBL2173434

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Binding
Inhibition of NHE1 in human platelet rich plasma assessed as reduction of propionate medium induced platelet swelling measured every 6 secs for 5 mins
ChEMBL ↗
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium/hydrogen exchanger 1 (CHEMBL2781) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat.
Huber JD, Bentzien J, Boyer SJ, Burke J, De Lombaert S, Eickmeier C, Guo X, Haist JV, Hickey ER, Kaplita P, Karmazyn M, Kemper R, Kennedy CA, Kirrane T, Madwed JB, Mainolfi E, Nagaraja N, Soleymanzadeh F, Swinamer A, Eldrup AB.
J Med Chem (2012) 55 : 7114 -7140
PubMed 22803959 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 6.82 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2170615 — — 1 7.64
CHEMBL2170639 — — 1 7.60
CHEMBL2170611 — — 1 7.55
CHEMBL2170610 BI 9627 — 1 7.51
CHEMBL2170609 — — 1 7.51
CHEMBL2170636 — — 1 7.50
CHEMBL2170638 — — 1 7.44
CHEMBL2170608 — — 1 7.32
CHEMBL2170633 — — 1 7.30
CHEMBL2170607 — — 1 7.30
CHEMBL2170603 — — 1 7.25
CHEMBL2170618 — — 1 7.21
CHEMBL2170635 — — 1 7.16
CHEMBL2170621 — — 1 7.11
CHEMBL2170606 — — 1 7.10
CHEMBL2170637 — — 1 7.10
CHEMBL2169894 — — 1 7.06
CHEMBL2170622 — — 1 7.06
CHEMBL2170632 — — 1 7.03
CHEMBL2170642 — — 1 6.96
CHEMBL2170617 — — 1 6.96
CHEMBL2170630 — — 1 6.96
CHEMBL2170616 — — 1 6.94
CHEMBL2170605 — — 1 6.90
CHEMBL2170628 — — 1 6.86
CHEMBL2170629 — — 1 6.82
CHEMBL2170627 — — 1 6.77
CHEMBL2105423 SABIPORIDE 2.0 1 6.76
CHEMBL2170643 — — 1 6.74
CHEMBL2170614 — — 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2170615 — IC50 = 23.0 nM 7.64
CHEMBL2170639 — IC50 = 25.0 nM 7.60
CHEMBL2170611 — IC50 = 28.0 nM 7.55
CHEMBL2170610 BI 9627 IC50 = 31.0 nM 7.51
CHEMBL2170609 — IC50 = 31.0 nM 7.51
CHEMBL2170636 — IC50 = 32.0 nM 7.50
CHEMBL2170638 — IC50 = 36.0 nM 7.44
CHEMBL2170608 — IC50 = 48.0 nM 7.32
CHEMBL2170633 — IC50 = 50.0 nM 7.30
CHEMBL2170607 — IC50 = 50.0 nM 7.30
CHEMBL2170603 — IC50 = 56.0 nM 7.25
CHEMBL2170618 — IC50 = 62.0 nM 7.21
CHEMBL2170635 — IC50 = 70.0 nM 7.16
CHEMBL2170621 — IC50 = 77.0 nM 7.11
CHEMBL2170637 — IC50 = 79.0 nM 7.10
CHEMBL2170606 — IC50 = 79.0 nM 7.10
CHEMBL2169894 — IC50 = 88.0 nM 7.06
CHEMBL2170622 — IC50 = 88.0 nM 7.06
CHEMBL2170632 — IC50 = 93.0 nM 7.03
CHEMBL2170642 — IC50 = 109.0 nM 6.96
CHEMBL2170617 — IC50 = 111.0 nM 6.96
CHEMBL2170630 — IC50 = 111.0 nM 6.96
CHEMBL2170616 — IC50 = 115.0 nM 6.94
CHEMBL2170605 — IC50 = 127.0 nM 6.90
CHEMBL2170628 — IC50 = 138.0 nM 6.86
CHEMBL2170629 — IC50 = 152.0 nM 6.82
CHEMBL2170627 — IC50 = 169.0 nM 6.77
CHEMBL2105423 SABIPORIDE IC50 = 172.0 nM 6.76
CHEMBL2170643 — IC50 = 184.0 nM 6.74
CHEMBL2170614 — IC50 = 189.0 nM 6.72
CHEMBL2170631 — IC50 = 200.0 nM 6.70
CHEMBL2170604 — IC50 = 201.0 nM 6.70
CHEMBL2170620 — IC50 = 214.0 nM 6.67
CHEMBL2170625 — IC50 = 221.0 nM 6.66
CHEMBL2170641 — IC50 = 241.0 nM 6.62
CHEMBL2170623 — IC50 = 241.0 nM 6.62
CHEMBL2170613 — IC50 = 266.0 nM 6.58
CHEMBL2170634 — IC50 = 269.0 nM 6.57
CHEMBL2170626 — IC50 = 353.0 nM 6.45
CHEMBL2170649 — IC50 = 368.0 nM 6.43
CHEMBL2170624 — IC50 = 416.0 nM 6.38
CHEMBL2170612 — IC50 = 432.0 nM 6.37
CHEMBL2170647 — IC50 = 495.0 nM 6.30
CHEMBL2170619 — IC50 = 498.0 nM 6.30
CHEMBL2170644 — IC50 = 539.0 nM 6.27
CHEMBL2170640 — IC50 = 950.0 nM 6.02
CHEMBL2170646 — IC50 = 989.0 nM 6.00
CHEMBL2170645 — IC50 = 1130.0 nM 5.95
CHEMBL2170650 — IC50 = 1586.0 nM 5.80
CHEMBL2170651 — IC50 = 3477.0 nM 5.46